| 02-09 |
A convenient method for screening sphingomyelinase inhibitors
Cayman’s Sphingomyelinase Inhibitor Screening Assay provides a convenient method for screening sphingomyelinase inhibitors. Cleavage of the sphingomyelin conjugate by SMase results in the release of a ceramide analog containing a free thiol which is detected by the fluorescent SMase Detector. This fluorescence is analyzed with an excitation wavelength of 375-385 nm and an emission wavelength of 510-520 nm.
|
700330 |
|
| 02-05 |
MyD88 is an adapter protein that links toll-like receptors (TLRs) and interleukin-1 receptors (IL-1Rs) with downstream signaling molecules. Homodimerization of MyD88 is a critical step in the signaling process and allows the recruitment and activation of the kinase IRAK. MyD88 exists as a homodimer when recruited to activate TLR/IL-receptors (TIR). The inhibitor peptide contains a sequence from the MyD88 TIR homodimerization domain. MyD88 monomer binds to this inhibitor peptide, thereby blocking Myd88 homodimerization. The MyD88 homodimerization inhibitory peptide contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permeable. The control peptide consists of only the PTD sequence.
|
13748 |
|
| 02-05 |
For immunochemical analysis of MyD88
Antigen:
synthetic peptide corresponding to human MyD88 amino acids 233-248
·
Host:
rabbit
·
Application(s):
WB
·
|
13746 |
|
| 02-05 |
For immunochemical analysis of NF-κB (p50)
Antigen:
a portion of amino acids 150-200 of human NF-κB (p50)
·
Clone designation:
2J10D7
·
Isotype:
IgG1κ
·
Application(s):
IHC and WB
·
|
13755 |
|
| 02-05 |
An aconitase inhibitor
Oxalomalic acid, formed by the condensation of oxaloacetate with glyoxylate in vivo, inhibits both aconitase and NADP-dependent isocitrate dehydrogenase in the conversion of citrate to isocitrate at concentrations as low as 1 mM. At 5 mM, oxalomalic acid inhibition of aconitase leads to a decrease in the binding activity of IRP1 and a decrease in glutamate secretion in cultured lens epithelial cells, retinal pigment epithelial cells, and neurons.
|
13521 |
|
| 02-05 |
An inhibitor of Ewing’s sarcoma tumors
YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 µM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5 to 2 µM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
|
13661 |
|
| 02-03 |
A dopamine precursor used to treat Parkinson’s Disease
L-DOPA is a metabolic precursor of dopamine that is capable of crossing the blood brain barrier. It is produced from L-tyrosine by trysosine hydroxylase and metabolized by catechol-O-methyl transferase (COMT) . In the brain L-DOPA is converted to dopamine. It is conventionally used to increase dopamine concentrations in the brain as a treatment for Parkinson’s disease and stroke recovery. However L-DOPA has a short half-life and is known to elevate homocysteine concentrations in plasma, which can be neurotoxic and induce oxidative damage.
|
13248 |
|
| 02-02 |
Analog of PGJ2
13,14-dihydro-16,16-difluoro PGJ2 is an analog of PGJ2. While its biological activities have not been evaluated, it should be noted that the addition of two electron-withdrawing fluorine atoms has been used to stabilize prostanoids and significantly delay degradation in vivo. Importantly, 13,14-dihydro PGE1 has activity that is comparable to that of PGE1, suggesting that this analog of PGJ2 could be biologically active.
|
13635 |
|
| 02-02 |
An internal standard for the quantification of 6,15-diketo-13,14-dihydro PGF1α
6,15-diketo-13,14-dihydro PGF1α is a metabolite of PGI2. It was shown to enhance intracellular cAMP and cholesterol catabolism in bovine arterial smooth muscle cells.
|
9000525 |
|
| 02-02 |
Selective EP1 antagonist
SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat. SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo. In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.
|
10011561 |
|
| 02-02 |
A potent RTK inhibitor
SU 11652 is a potent, cell-permeable, and ATP-competitive inhibitor of the tyrosine kinase activity of several GFRs, including platelet-derived GFR (PDGFR-β; IC50 = 3 nM), vascular endothelial GFR (VEGFR-2; IC50 = 27 nM), and fibroblast GFR (FGFR1; IC50 = 170 nM), but not epidermal GFR (IC50 > 20 μM). SU 11652 also potently inhibits wild-type Kit in mast cells (IC50 = 50 nM) and stops cell cycling while inducing apoptosis in cells expressing constitutively-active kit mutants. Furthermore SU 11652 reduces angiogenesis induced by estrogen in mice.
|
13577 |
|
| 01-29 |
A carotenoid with anti-obesity actions
Fucoxanthin is a carotenoid that occurs naturally in certain algae. It significantly reduces abdominal white adipose tissue (WAT) in mice and rats when included in their diet. Fucoxanthin also increases the amount of mitochondrial uncoupling protein 1 (UCP1), a fatty acid-stimulated protein involved in respiration and thermogenesis in WAT of mice and rats. In KK-Ay mice, which are used to model obese type 2 diabetics with hyperinsulinemia, fucoxanthin reduces WAT gain and also decreases blood glucose and plasma insulin levels.
|
13068 |
|
| 01-27 |
Analog of PGD2
13,14-dihydro-16,16-difluoro PGD2 is an analog of PGD2. While its biological activities have not been evaluated, it should be noted that the addition of two electron-withdrawing fluorine atoms has been used to stabilize prostanoids and significantly delay degradation in vivo. Importantly, 13,14-dihydro PGE1 has activity that is comparable to that of PGE1, suggesting that this analog of PGD2 should be biologically active.
|
13612 |
|
| 01-27 |
Analog of PGF2α
13,14-dihydro-16,16-difluoro PGF2α is an analog of PGF2α. While its biological activities have not been evaluated, it should be noted that the addition of two electron-withdrawing fluorine atoms has been used to stabilize prostanoids and significantly delay degradation in vivo. Importantly, 13,14-dihydro PGE1 has activity that is comparable to that of PGE1, suggesting that this analog of PGF2α could be biologically active.
|
13609 |
|
| 01-27 |
Potent, selective inhibitor of Rho kinase II (ROCK-II)
Rho Kinase Inhibitor IV is a selective and potent Rho kinase inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil hydrochloride) and exhibits better specificity. Thus, it poorly inhibits calcium/calmodulin kinase II, protein kinase G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 > 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).
|
13332 |
|
| 01-27 |
Inhibitor of FAAH
PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment. PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.
|
13279 |
|
| 01-25 |
Selective inhibitor of PI3Kγ
AS 041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 ). When tested at 1.0 μM, it shows little or no activity against 38 other common kinases. When given orally to mice, AS 041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.35 mg/kg for AS 041164 versus 81.59 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.
|
13622 |
|
| 01-25 |
An antibacterial and immunosuppressant
Celastramycin A is a bioactive compound isolated from endophytic bacteria living in plants of the Celastraceae family. This benzoyl pyrrole inhibits the growth of bacteria and mycobacteria, with a minimal inhibitory concentration as low as 0.05 μg/ml. Celastramycin A also suppresses the production of IL-8 in human umbilical vein endothelial cells as stimulated by TNF-α (IC50 = 0.01 μg/ml).
|
13519 |
|
| 01-25 |
Antigen:
human CMKLR1 amino acids 358–371 (NERTSMNERETGML)
·
Host:
rabbit
·
Peptide sequence:
WB, FC, and IHC
·
|
10325 |
|
| 01-21 |
Estrogen receptor modulator
Tamoxifen is a selective estrogen receptor modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is effective in the treatment of early breast cancer to prevent tumor growth. Importantly, tamoxifen acts as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women. Also, tamoxifen is a partial ER agonist in uterine tissues and increases the risk of endometrial carcinoma.
|
13258 |
|
| 01-20 |
An internal standard for the quantification of PEA
|
9000551 |
|
| 01-19 |
An H2S-releasing latanoprost analog
ACS 67 is an analog of latanoprost (free acid) that contains a hydrogen sulfide releasing component conjugated to the latanoprost carboxyl group. In glaucomatous pigmented rabbits, ACS 67 reduced intra-ocular pressure (IOP) more rapidly and to a greater extent than latanoprost (15 versus 25.5 mm Hg at 4 hours) at a dose of 0.005% for each compound. ACS 67 also increased the levels of reduced glutathione and cGMP in the aqueous humor of glaucomatous pigmented rabbits better than latanoprost.
|
13619 |
|
| 01-19 |
For immunochemical analysis of Akt3
Antigen:
synthetic peptide from human Akt3 amino acids 119-136 (CSPTSQIDNIGEEEMDAS); this sequence is identical in human, murine, rat, ovine, canine, and chicken
·
Clone designation:
66C1247.1
·
Host:
mouse
·
Isotype:
IgG1
·
Application(s):
WB
·
|
13736 |
|
| 01-19 |
Antigen:
human GPR17 amino acids 351-367 (SFEGKTNESSLSAKSEL)
·
Host:
rabbit
·
Peptide sequence:
WB, FC, and ICC
·
|
10136 |
|
| 01-19 |
Antigen:
human GPR55 amino acids 207-219 (ILLGRRDHTQDWV)
·
Host:
rabbit
·
Application(s):
WB, FC, and ICC
·
|
10224 |
|
| 01-18 |
For immunochemical analysis of Akt3
Antigen:
synthetic peptide from human Akt3 amino acids 119-136; this sequence is identical in human, murine, and rat
·
Host:
rabbit
·
Application(s):
WB
·
|
13737 |
|
| 01-18 |
Peptide to block Akt1, Akt2, and Akt3 kinase activity
Akt is a protein kinase that plays a central role in inhibiting apoptosis through promoting cell survival. Activated Akt functions by phosphorylating downstream targets in survival signaling pathways. TCL1 (a proto-oncogene underlying human T-cell prolymphocytic leukemia) interacts with Akt through an N-terminal pleckstrin homology (PH) domain and functions as an Akt kinase co-activator. This inhibitory peptide interacts with Akt. The peptide binds to the PH domain of Akt and inhibits Akt1, Akt2, and Akt3 kinase activity. The Akt (Isoforms 1, 2, 3) inhibitory peptide also contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permeable. The control peptide consists of only the PTD sequence.
|
13738 |
|
| 01-18 |
For immunochemical analysis of FoxP3/Scurfin
Antigen:
synthetic peptide corresponding to the exon 2 deletion site was used as immunogen
·
Host:
rabbit
·
Application(s):
IHC and WB
·
|
13739 |
|
| 01-18 |
For immunochemical analysis of FoxP3Δ2
Antigen:
synthetic peptide corresponding to the exon 2 deletion site
·
Clone designation:
16J4G6
·
Host:
Mouse
·
Isotype:
IgMκ
·
Application(s):
WB
·
|
13744 |
|
| 01-18 |
For immunochemical analysis of FoxP3Δ2
Antigen:
synthetic peptide corresponding to the exon 2 deletion sit
·
Clone designation:
16J4G6
·
Host:
mouse
·
Isotype:
IgMκ
·
Application(s):
WB
·
|
13743 |
|
| 01-15 |
A flow cytometric assay to assess cell proliferation
Cayman’s CFSE Cell Division Assay Kit provides an easy to use format for labeling and tracing cells through successive cell divisions which can be used to study the induction and inhibition of cell division in any in vitro model. The kit contains sufficient reagents for labeling and analyzing 100 cell samples by flow cytometry. CFSE can also be combined with any fluorochrome compatible with fluorescein for use in flow cytometry.
|
10009853 |
|
| 01-14 |
High-affinity cannabinoid receptor agonist
JWH 019 is a cannabimimetic indole that shows a high-affinity for both the central cannabinoid (CB1) and the peripheral cannabinoid (CB2) receptors. The affinities of JWH 019 for both CB1 (Ki = 9.8 nM) and CB2 (Ki = 5.6 nM) are superior to those of the traditional cannabinoid, Δ9-tetrahydrocannabinol (Δ9-THC; Ki values of 40.7 and 36.4 nM for CB1 and CB2, respectively).
|
13633 |
|
| 01-14 |
High-affinity cannabinoid receptor agonist
JWH 250 is a cannabimimetic indole that shows a high-affinity for both the central cannabinoid (CB1) and the peripheral cannabinoid (CB2) receptors. The affinities of JWH 250 for both CB1 (Ki = 11 nM) and CB2 (Ki = 33 nM) are comparable to those of the traditional cannabinoid, Δ9-tetrahydrocannabinol (Δ9-THC; Ki = 40.7 and 36.4 nM, respectively).
|
13634 |
|
| 01-13 |
An internal standard for the quantification of linoleoyl ethanolamide by GC- or LC-MS
|
9000553 |
|
| 01-12 |
For immunochemical analysis of Akt2/3
Antigen:
synthetic peptide from human Akt2 amino acids 319-331; this sequence is 100% homologus in Akt3
·
Host:
rabbit
·
|
13735 |
|
| 01-12 |
For immunochemical analysis of Akt2
Antigen:
synthetic peptide from human Akt2 amino acids 106-123
·
Clone designation:
95C567.1.2
·
Host:
mouse
·
Isotype:
IgM
·
Application(s):
WB
·
|
13734 |
|
| 01-12 |
Neruroprotective drug
Dimebon is an orally-available drug, approved in Russia for use as a non-selective antihistamine, that has shown promise in the treatment of neurodegenerative diseases, including Alzheimer’s and Huntington’s disease. In addition to preventing the onset and progression of disease by being neuroprotective, dimebon appears to promote clinical improvement by increasing cognitive function. At the cellular level, dimebon appears to have diverse effects, inhibiting the neurotoxic action of β-amyloid and blocking L-type calcium channels, inhibiting NMDA-type glutamate receptors, and preventing mitochondrial leakage.
|
9000556 |
|
| 01-12 |
An internal standard for the quantification of OEA by GC- or LC-MS
|
9000552 |
|
| 01-11 |
For immunochemical analysis of Akt1 (Phospho-Ser473)
Antigen:
synthetic peptide from human Akt1 containing phospho-serine473
·
Clone designation:
104A282
·
Host:
mouse
·
Isotype:
IgG2κ
·
Application(s):
IP and WB
·
|
13733 |
|
| 01-11 |
For immunochemical analysis of Akt1
Antigen:
synthetic peptide from human Akt1 amino acids 464-477; this peptide sequence is identical in human, murine, chicken, and frog
·
Host:
rabbit
·
Application(s):
WB
·
|
13732 |
|
| 01-07 |
Source:
recombinant N-terminal Histidine-tagged SET8 amino acids 190-352, purified from E. coli, NP-065115
·
Mr:
21.1 kDa
·
|
10319 |
|
| 01-06 |
A convenient method of detecting ALT activity in serum, plasma, tissue samples, and cell lysates
Cayman’s Alanine Transaminase Assay Kit provides a convenient method of detecting ALT activity in serum, plasma, tissue samples, and cell lysates. Measurement of the ALT activity is carried out by monitoring the rate of NADH oxidation in a coupled reaction system employing lactate dehydrogenase (LDH). The oxidation of NADH to NAD+ is accompanied by a decrease in absorbance at 340 nm. Under circumstances in which the ALT activity is rate limiting, the rate decrease is directly proportional to the ALT activity in the sample.
|
700260 |
|
| 01-06 |
Non-selective NSAID
Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) that non-selectively and reversibly inhibits both isoforms of cyclooxygenase (COX; IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively). It has an extended half-life of about 40 hours, which allows once daily administration leading to sustained plasma and tissue levels. In addition to its anti-inflammatory effects, piroxicam is an effective analgesic that has been used extensively in the treatment of arthritis. It has also been used to inhibit COX activity for treatment of certain cancers in animals. As with other NSAIDs, the extended use of piroxicam results in damage to the gastrointestinal lining.
|
13368 |
|
| 01-06 |
Source:
Recombinant N-terminal GST-tagged SIRT4 purified from E. coli
·
Mr:
61.9 kDa
·
|
10317 |
|
| 01-05 |
A cell-based screening assay based on novel transfection (STEP™) technology
Cayman’s Melanocortin 3 Receptor STEP™ Reporter Assay Kit (Luminescence) consists of a 96-well plate coated with both MC3R and Secretory Alkaline Phosphatase (SEAP) reporter constructs (MC3R STEP™ Plate). Cells grown on the STEP™ complex will express MC3R at the cell surface. Binding of agonists to MC3R initiates a signal transduction cascade resulting in expression of SEAP which is secreted into the cell culture media. Aliquots of media are removed at timed intervals, beginning at approximately six hours, and SEAP activity is measured following addition of a luminescence-based alkaline phosphatases substrate provided in the kit. The kit is simple to use and can be easily adapted to high throughput screening for therapeutic compounds regulating the activation of MC3R. A MC3R agonist, α-MSH (α-melanocyte-stimulating hormone), is included in the kit for use as a positive control. The kit provides sufficient reagent to measure SEAP activity at three time points, using the black plates included.
|
600180 |
|
| 01-05 |
A cell-based screening assay based on novel transfection (STEP™) technology
Cayman’s Melanocortin 4 Receptor STEP™ Reporter Assay Kit (Luminescence) consists of a 96-well plate coated with both MC4R and Secretory Alkaline Phosphatase (SEAP) reporter constructs (MC4R STEP™ Plate). Cells grown on the STEP™ complex will express MC4R at the cell surface. Binding of agonists to MC4R initiates a signal transduction cascade resulting in expression of SEAP which is secreted into the cell culture media. Aliquots of media are removed at timed intervals, beginning at approximately six hours, and SEAP activity is measured following addition of a luminescence-based alkaline phosphatases substrate provided in the kit. The kit is simple to use and can be easily adapted to high throughput screening for therapeutic compounds regulating the activation of MC4R. A MC4R agonist, α-MSH (α-melanocyte-stimulating hormone), is included in the kit for use as a positive control. The kit provides sufficient reagent to measure SEAP activity at three time points, using the black plates included.
|
600190 |
|
| 12-22 |
Source:
Full length (2-400 aa) recombinant N-terminal hexahistidine tagged SIRT7, expressed in E. coli
·
Mr:
49.3 kDa
·
|
10316 |
|
| 12-22 |
Biologically active oxidative derivative of linoleic acid
trans-EKODE-(E)-Ib is a biologically active peroxidation product of linoleic acid that is characterized, structurally, by having a trans carbon-carbon double bond between the 9-keto and 12,13-epoxy groups. It activates an antioxidant response element (ARE) in neuronal cells and induces the expression of ARE-regulated cytoprotective genes like NQO1. This EKODE also stimulates the synthesis of aldosterone and corticosterone in adrenal cells when supplied at 1-5 μM. This effect appears to be mediated by a rise in intracellular calcium.
|
10004224 |
|
| 12-17 |
For the immunochemical detection of proteins containing MetO residues by western blotting
Cayman’s Methionine Sulfoxide (MetO) Immunoblotting Kit contains reagents needed for the immunochemical detection of proteins containing MetO residues by western blotting. MetO-containing samples of interest include those from cell or tissue lysates as well as semi-pure or purified proteins. Samples may be prepared with reducing or non-reducing sample buffer prior to SDS-PAGE and tested along side one SDS-PAGE well designated for the provided positive control. The MetO Polyclonal Antibody was isolated from rabbit serum generated after immunization with a oxidized corn protein (MetO-DZS18) rich in methionine. This polyclonal antibody is specific for protein methionine sulfoxide.
|
600160 |
|
| 12-10 |
For detection of aldehyde sites in cells
Cayman’s Aldehyde Site (DNA and Protein) Detection Kit employs an aldehyde reactive probe (ARP), O-(biotinylcarbazoylmethyl) hydroxylamine, as a probe to detect aldehyde sites in cells. Epigallocatechin Gallate (EGCG), a compound known to react with culture medium to generate hydrogen peroxide (H2O2) and cause DNA damage, is included to be used as a positive control. The kit is easy to use and can be easily adapted to high throughput screening for compounds imposing oxidative stress on cells or organisms.
|
600170 |
|
| 12-10 |
A convenient fluorescence-based method for screening SIRT2 inhibitors or activators
Cayman’s SIRT2 Direct Fluorescent Screening Assay provides a convenient fluorescence-based method for screening SIRT2 inhibitors or activators. The procedure requires only two easy steps, both performed in the same microplate. In the first step, the substrate, which comprises the p53 sequence Gln-Pro-Lys-Lys(ε-acetyl)-AMC, is incubated with human recombinant SIRT2 along with its cosubstrate NAD+. Deacetylation sensitizes the substrate such that treatment with the Developer in the second step releases a fluorescent product. The fluorophore can be analyzed with an excitation wavelength of 350-360 nm and an emission wavelength of 450-465 nm.
|
700280 |
|
| 12-07 |
Isomer of bimatoprost
15(R)-Bimatoprost is an isomer of bimatoprost, characterized by an inverted (β) hydroxyl group at C-15. While this isomer has not been characterized, the comparable inversion of 15-hydroxyl groups, from (S) to (R), on other PGF2α analogs typically decreases, but does not eliminate, activity.
|
10008127 |
|
| 12-07 |
Inhibitor of xanthine oxidase
Allopurinol is an isomer of hypoxanthine that inhibits xanthine oxidoreductase (IC50 values between 0.2 and 50 μM, depending on assay and cell type). In vivo, allopurinol has been reported to effectively and safely lower serum and urinary uric acid levels and is also reported to be effective in the treatment of gout and hyperuricemia. Allopurinol is rapidly metabolized in vivo to the xanthine analog oxypurinol; which is a metabolite that clearly augments the therapeutic effect of allopurinol.
|
10012597 |
|
| 12-04 |
Sex pheromone in Drosophila
7(Z),11(Z)-Pentacosadiene is a 25-C hydrocarbon that is found in low abundance on cuticles of mature Drosophila females. Depletion of a female-specific elongase (eloF), which leads to an increase in 7(Z),11(Z)-pentacosadiene along with a parallel decrease in 7,11-nonacosadiene, significantly reduces copulation in Drosophila. This raises the possibility that 7(Z),11(Z)-pentacosadiene may act as an anti-aphrodisiac.
|
9000531 |
|
| 12-04 |
For immunochemical detection of acetylated lysine
Antigen:
acetylated KLH
·
Host:
rabbit
·
Application(s):
WB, IP, ELISA, and IF
·
|
13725 |
|
| 12-04 |
For immunochemical detection of acetylated lysine
Antigen:
acetylated KLH
·
Host:
rabbit
·
Application(s):
WB, IP, ELISA, and IF
·
|
13726 |
|
| 12-04 |
Inhibitor of 5-lipoxygenase
CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM). It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC50 = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC50 = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.
|
13381 |
|
| 12-04 |
For screening of variety of fatty acids
This screening plate contains a variety of fatty acids with diverse biological activities.
|
10504 |
|
| 12-04 |
For immunochemical detection of Kir2.3
Antigen:
fusion protein amino acids 390-445 of human Kir2.3
·
Clone designation:
S25-35
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB and IHC
·
|
13716 |
|
| 12-04 |
For immunochemical detection of Kv3.1b
Antigen:
fusion protein amino acids 437-585 of rat Kv3.1b
·
Clone designation:
Mouse
·
Host:
S16B-8
·
Isotype:
IgG1
·
Application(s):
WB and IHC
·
|
13717 |
|
| 12-04 |
For immunochemical detection of methylated lysine
Antigen:
methylated KLH
·
Host:
rabbit
·
Application(s):
WB, IP, and ELISA
·
|
13728 |
|
| 12-04 |
For immunochemical detection of methylated lysine
Antigen:
methylated KLH
·
Host:
rabbit
·
Application(s):
WB and ELISA
·
|
13729 |
|
| 12-04 |
For immunochemical detection of Nav1.7
Antigen:
fusion protein amino acids 1,751-1,946 of rat Nav1.7
·
Clone designation:
S68-6
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, and ICC
·
|
13718 |
|
| 12-04 |
An internal standard for the quantification of palmitoleic acid
Palmitoleic acid is an ω-7 monounsaturated fatty acid that is a common constituent of the triglycerides of human adipose tissue. It is found mainly in animal fats, particularly in fish and marine mammals, and is also present in the seeds of plants of the Proteaceae family. In contrast to a diet enriched with oleic acid, palmitoleic acid-based diets raise low-density lipoprotein (LDL) cholesterol and lower high-density lipoprotein (HDL) cholesterol much like that of a saturated fatty acid, even when dietary intake of cholesterol is maintained at a low level.
|
9000431 |
|
| 12-04 |
Compound from traditional medicine with reported antifungal, anticancer actions
Pseudolaric acid B (PAB) is a diterpene acid isolated from the bark of P. kaempferi, a traditional Chinese medicinal plant. PAB has antifungal activities, consistent with its traditional use in the treatment of dermatological fungal infections. Moreover, PAB has diverse effects that are relevant to cancer therapy, including inducing apoptosis of cancer cells (IC50 = ~1 μM), preventing angiogenesis, and inhibiting tumor growth in vivo.
|
13527 |
|
| 12-04 |
A convenient method for screening human SET7/9 inhibitors
Cayman’s SET7/9 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET7/9 inhibitors. The transfer of the methyl group from SAM by SET7/9 to the acceptor peptide (TAF 10) generates S-adenosylhomocysteine, which is rapidly converted to S-ribosylhomocysteine and adenine by adenosylhomocysteine nucleosidase. This rapid conversion prevents the buildup of adenosylhomocysteine and its feedback inhibition on the methylation reaction. Finally, the adenine is converted to hypoxanthine by adenine deaminase, which in turn is converted to urate and hydrogen peroxide (H2O2). The reaction between H2O2 and ADHP (10-acetyl-3,7-dihydroxyphenoxazine) produces the highly fluorescent compound resorufin. Resorufin fluorescence is analyzed using an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
|
700270 |
|
| 12-04 |
For immunochemical detection of TRPC4
Antigen:
synthetic peptide amino acids 930-947 of rat TRPC4
·
Clone designation:
S77-15
·
Host:
Mouse
·
Isotype:
IgG2b
·
Application(s):
WB, IP, and ICC
·
|
13719 |
|
| 12-04 |
For immunochemical detection of TRPM7
Antigen:
fusion protein amino acids 1,817-1,863 of murine TRPM7
·
Clone designation:
S74-25
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, and ICC
·
|
13720 |
|
| 12-04 |
For immunochemical detection of TRPV3
Antigen:
amino acids 458-474 of rat TRPV3
·
Clone designation:
S15-4
·
Host:
Mouse
·
Isotype:
IgG2a
·
Application(s):
WB, IP, and ICC
·
|
13721 |
|
| 12-04 |
For immunochemical detection of ubiquitin
Antigen:
native bovine ubiquitin conjugated to KLH
·
Clone designation:
5B9-B3
·
Host:
Mouse
·
Isotype:
IgG2aκ
·
Application(s):
WB and ELISA
·
|
13722 |
|
| 12-04 |
For immunochemical detection of ubiquitin
Antigen:
native bovine ubiquitin conjugated to KLH
·
Clone designation:
6C11-B3
·
Host:
Mouse
·
Isotype:
IgG2aκ
·
Application(s):
WB and ELISA
·
|
13723 |
|
| 12-04 |
For immunochemical detection of ubiquitin
Antigen:
native bovine ubiquitin conjugated to KLH
·
Host:
rabbit
·
Application(s):
WB, IP, and ChIP
·
|
13724 |
|
| 12-03 |
Analog of PGE1
13,14-dihydro-16,16-difluoro PGE1 is an analog of PGE1. 13,14-dihydro PGE1 is a biologically active metabolite of PGE1, inhibiting platelet aggregation with comparable potency to the parent compound. The addition of two electron-withdrawing fluorine atoms, which should stabilize the molecule against hydrolytic cleavage, may be expected to delay degradation in vivo.
|
9000405 |
|
| 12-03 |
Sex pheromone in Drosophila
7(Z)-Pentacosene is an unsaturated cuticular hydrocarbon that acts as a contact sex pheromone in fruit flies. In different species and genotypes of Drosophila, it can be found on both males and females. Pentacosene may stimulate copulation either by itself at high concentrations or when combined with other alkenes. Interestingly, the absolute level of pentacosene increases in Drosophila females immediately after copulation.
|
9000530 |
|
| 12-03 |
An inhibitor of G9a histone methyltransferase
BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.
|
13124 |
|
| 12-03 |
A farnesoid X receptor antagonist
Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR both in vitro and in vivo. The cis stereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50 value of 15 µM. By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.
|
10011296 |
|
| 12-03 |
Inhibitor of HDACs
(S)-HDAC-42 is a potent inhibitor of HDACs (IC50 = 16 nM in vitro). It decreases the viability of prostate cancer cell lines (IC50 = 0.40 μM), increasing the expression of p21 and the acetylation of histone H3 while decreasing the phosphorylation of Akt and the expression of Bcl-XL. (S)-HDAC-42 also strongly suppresses the growth of PC-3 tumor xenografts, reducing levels of phospho-Akt and Bcl-XL protein in tumors.
|
13277 |
|
| 12-03 |
Antigen:
murine recombinant soluble epoxide hydrolase
·
Host:
rabbit
·
Application(s):
WB
·
|
13560 |
|
| 12-03 |
A tankyrase inhibitor
XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively. By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.
|
13596 |
|
| 12-02 |
An internal standard for the quantification of a PGE1 analog
It is intended for use as an internal standard for the quantification of 13,14-dihydro-15(R,S)-hydroxy-16,16-difluoro Prostaglandin E1 by GC- or LC-mass spectrometry (MS).
|
9000406 |
|
| 12-02 |
For immunochemical detection of HCN4
Antigen:
fusion protein amino acids 1,019-1,108 (cytoplasmic C-terminus) of rat HCN4
·
Clone designation:
S114-10
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, ICC, and IHC
·
|
13709 |
|
| 12-02 |
For immunochemical detection of KCNQ1
Antigen:
fusion protein amino acids 2-101 of human KCNQ1
·
Clone designation:
S37A-10
·
Host:
mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, IHC, and ICC
·
|
13711 |
|
| 12-02 |
For immunochemical detection of KCNQ2
Antigen:
fusion protein amino acids 1-59 of human KCNQ2
·
Clone designation:
S26A-23
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, IHC, and ICC
·
|
13712 |
|
| 12-02 |
For immunochemical detection of KCNQ4
Antigen:
fusion protein amino acids 2-77 of human KCNQ
·
Clone designation:
S43-6
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, and ICC
·
|
13713 |
|
| 12-02 |
For immunochemical detection of Kir2.1
Antigen:
fusion protein amino acids 41-64 and 189-428 of murine Kir2.1
·
Clone designation:
S21-32
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB and IHC
·
|
13714 |
|
| 12-02 |
For immunochemical detection of Kir2.2
Antigen:
fusion protein amino acids 362-427 of murine Kir2.2
·
Clone designation:
S24-1
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB and IHC
·
|
13715 |
|
| 12-02 |
An internal standard for the quantification of SAH
S-Adenosyl-L-homocysteine-d4 (SAH-d4) contains four deuterium atoms at the 3, 3’, 4, and 4’ positions. It is intended for use as an internal standard for the quantification of SAH by GC- or LC-mass spectrometry (MS).
|
9000372 |
|
| 12-01 |
Pro-apoptotic analog of resveratrol
CAY10616 is an analog of resveratrol which potently induces apoptosis in promyelocytic leukemia HL-60 cells (IC50 = 40 nM, vs. 50 μM for resveratrol). In addition, CAY10599 induces apoptosis (IC50 = 30 nM) in HL60R, a cell line derived from HL-60 that expresses a multidrug-resistance phenotype (resistant to daunorubicin, etoposide, and citarabine).
|
13291 |
|
| 12-01 |
For immunochemical detection of HCN1
Antigen:
fusion protein amino acids 778-910 (cytoplasmic C-terminus) of rat HCN1
·
Clone designation:
S70-28
·
Host:
mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, IHC, and ICC
·
|
13705 |
|
| 12-01 |
For immunochemical detection of HCN2
Antigen:
fusion protein amino acids 761-863 (cytoplasmic C-terminus) of rat HCN2
·
Clone designation:
S71-37
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IP, IHC, and ICC
·
|
13707 |
|
| 12-01 |
For immunochemical detection of HCN3
Antigen:
fusion protein amino acids 660-779 (cytoplasmic C-terminus) of murine HCN3
·
Clone designation:
S141-28
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, ICC, and IHC
·
|
13708 |
|
| 12-01 |
An endogenous signaling lipid
N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 µg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 µM).
|
10009020 |
|
| 12-01 |
A farnesoid X receptor antagonist
Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR both in vitro and in vivo. The trans stereoisomer of guggulsterone, (Z)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50 value of 17 µM. By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet. While both cis and trans stereoisomers have been shown to directly decrease hepatic cholesterol, the Z isomer is the most studied. (Z)-Guggulsterone demonstrates antitumor-promoting effects inhibiting both constitutive and interleukin-6-induced STAT3 activation in human multiple myeloma cells and suppressing the VEGF-VEGF/R2-Akt signaling axis in DU145 human prostate cancer cells.
|
71800 |
|
| 11-25 |
Antagonist of the PGE2 receptor EP1
GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM). It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels. Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species. In a rat model of chronic inflammatory joint pain, G W 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.
|
10010410 |
|
| 11-25 |
For immunochemical analysis of SET7/9
Antigen:
human SET7/9 amino acids 131-145 and 336-352
·
Host:
rabbit
·
Application(s):
WB
·
|
13731 |
|
| 11-25 |
A sensitive tool for assaying neutral and acidic sphingomyelinase activity
Cayman’s Sphingomyelinase (SMase) Assay provides a simple, reproducible, and sensitive tool for assaying neutral and acidic sphingomyelinase activity from tissue homogenates, cell lysates, serum, saliva, and urine. The SMase Assay utilizes a coupled enzymatic reaction to monitor SMase activity. SMase hydrolyzes sphingomyelin to yield ceramide and phosphorylcholine. Alkaline phosphatase hydrolyzes phosphorylcholine forming choline. Choline is then oxidized by choline oxidase to yield betaine and H2O2. Finally, H2O2, in the presence of horseradish peroxidase (HRP), reacts with 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) in a 1:1 stoichiometry to generate the highly fluorescent product resorufin. Resorufin fluorescence is analyzed with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
|
10006964 |
|
| 11-23 |
For immunochemical analysis of TLR12
Antigen:
murine TLR12 amino acids 911-926
·
Host:
Rabbit
·
Application(s):
WB and FC (intracellular)
·
|
13586 |
|
| 11-23 |
For immunochemical analysis of TLR7
Antigen:
synthetic peptide from human TLR7 within the region of amino acids 706-728
·
Host:
rabbit
·
Application(s):
WB, FC (intracellular and cell surface), IHC (frozen and paraffin), ICC, and IP
·
|
13591 |
|
| 11-16 |
Stimulator of soluble guanylate cyclase
BAY-41-8543 is a heme-dependent stimulator of sGC, increasing the activity of recombinant sGC dose-dependently, from 0.1 nM to 100 μM, up to 92-fold. Surprisingly, NO donors synergize with BAY-41-8543 in stimulating recombinant sGC. BAY-41-8543 relaxes vessels and inhibits platelet aggregation in vitro at nM concentrations. In vivo, BAY-41-8543 decreases blood pressure dose-dependently, prolongs bleeding time, and reduces thrombosis. Inhalation of microparticles containing BAY-41-8543 increases pulmonary vasodilation without changing mean arterial pressure, suggesting that agonists of sGC may be efficacious in treating pulmonary hypertension.
|
10011131 |
|
| 11-16 |
Inhibitor of calcium release-activated calcium channels
YM-58483 is a potent inhibitor of CRAC channels, blocking thapsigargin-induced sustained calcium influx, Th2 cytokine production, and NF-AT-driven promoter activity in T lymphocytes (IC50 = 100 nM). YM-58483 also inhibits lung interleukin-4 and cysteinyl leukotriene generation as well as airway eosinophil infiltration in animal models of asthma.
|
13246 |
|
| 11-12 |
For immunochemical detection of Cav1.3
Antigen:
fusion protein amino acids 859-875 (N-terminal) of human Cav1.3
·
Clone designation:
S48A-9
·
Host:
mouse
·
Isotype:
IgG2a
·
Application(s):
WB, IHC, and ICC
·
|
13706 |
|
| 11-12 |
For immunochemical detection of Cav3.2
Antigen:
fusion protein amino acids 1,019-1,293 (II-III loop) human Cav3.2
·
Clone designation:
S55-10
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IHC, and ICC
·
|
13704 |
|
| 11-12 |
Irreversible cysteine protease inhibitor
E-64 is a natural, potent and irreversible inhibitor of cysteine proteases. Its IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively. E-64 also inhibits papain, calpain, and cathepsins B and H, but not serine proteases (e.g., plasmin, trypsin, tissue kallikrein) or aspartic proteases (e.g., pepsin). The mode of action involves the formation of a thioether linkage between E-64 and the thiol group of the protease; E-64 does not react with the functional thiol group of non-protease enzymes (e.g., creatine kinase, L-lactate hydrogenase). While E-64 is usually used in biochemical assays, it can also be used in intact cells at higher (μM) concentrations.
|
10007963 |
|
| 11-12 |
For immunochemical analysis of TLR10
Antigen:
synthetic peptide from the extracellular domain of human TLR10
·
Clone designation:
158C1114
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB and FC (intracellular and cell surface)
·
|
13584 |
|
| 11-12 |
For immunochemical analysis of TLR11
Antigen:
murine TLR11 amino acids 911-926
·
Host:
rabbit
·
Application(s):
WB and FC (intracellular)
·
|
13585 |
|
| 11-11 |
96-Well assay for measurement of ATF2 (Phospho-Thr69,71)
Cayman’s ATF2 (Phospho-Thr69,71) Transcription Factor Assay is a non-radioactive, sensitive method for detecting specific transcription factor DNA binding activity in nuclear extracts. A 96-well enzyme-linked immunosorbent assay (ELISA) replaces the cumbersome radioactive electrophoretic mobility shift assay (EMSA). A specific double-stranded DNA (dsDNA) sequence containing the cAMP-response element (CRE) is immobilized onto the wells of a 96-well plate. ATF2 contained in a nuclear extract, binds specifically to the CRE. The activated ATF2 transcription factor complex is detected by addition of a specific primary antibody directed against the phospho-Thr69,71 epitope on ATF2. A secondary antibody conjugated to HRP is added to provide a sensitive colorimetric readout at 450 nm.
|
600130 |
|
| 11-11 |
Inhibitor of sphingosine N-acyltransferase; mycotoxin; food contaminant
Fumonisin B2 is a mycotoxin originally isolated from F. moniliforme, a prevalent fungus of corn and other grains. Fumonisins cause food poisoning in livestock and humans following the consumption of Fusarium-infested corn. Fumonisin B2, like fumonisin B1 (Catalog No. 62580), structurally resembles sphingosine and, at 1 μM, inhibits sphingosine N-acyltransferase (>90%) in hepatocytes. Fumonisins induce apoptosis via altered sphingolipid metabolism, resulting in hepatotoxicity and nephrotoxicity. It is now known that fumonisins are produced by fungi other than F. moniliforme and occur as contaminants in a wide variety of foods.
|
13227 |
|
| 11-11 |
Stable prostacyclin analog
Taprostene is a stable prostacyclin (PGI2) analog and agonist of the prostacyclin receptor, IP. It does not activate the PGE2 receptor EP4, which, like IP, promotes vascular smooth muscle relaxation when stimulated. Taprostene has been used extensively to study the role of the IP receptor in tissue preparations and in vivo. It has also been used in the screening and evaluation of potential IP antagonists.
|
10011348 |
|
| 11-10 |
A biotinylated spin trap
DEPMPO-biotin is a biotinylated form of DEPMPO which retains the outstanding persistency of its adducts. The biotin moiety offers an effective means for monitoring biodistribution in cells, tissues, and organs when used with an avidin-conjugated reporter. Importantly, DEPMPO-biotin binds free radicals, such as S-nitroso groups, on proteins, producing adducts that can be analyzed via the biotin tag. This direct labeling of S-nitrosothiols (SNO) thus serves as an effective alternative to the more cumbersome biotin-switch method for monitoring SNO formation.
|
13251 |
|
| 11-10 |
Natural resveratrol analog
Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. It is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. At higher concentrations, rhapontigenin inhibits the proliferation of Hep-G2 and HL-60R cancer cell lines (IC50 = 48 μM).
|
13293 |
|
| 11-09 |
Antibiotic used to select genetically-engineered cells
G-418 Sulfate is an aminoglycosidic antibiotic that is related to gentamicin. It is toxic to both prokaryotic and eukaryotic cells, as it blocks protein elongation during translation. G-418 is commonly used for the selection of cells that are genetically engineered with a plasmid containing the neo (neor) gene, which provides resistance to G-418. In mammalian cells, selection is commonly performed using 400 mg/L G-418, followed by 200 mg/L for culture maintenance; optimal concentrations may depend on cell type or plasmid and should be empirically determined.
|
13200 |
|
| 11-09 |
An easy tool for studying HDAC activity modulators in whole cells
Cayman’s HDAC Cell-Based Assay Kit provides an easy tool for studying HDAC activity modulators in whole cells. By using a cell-permeable HDAC substrate, the activity of various protein lysine-specific deacetylases including HDAC1-containing complexes can be measured in intact cells in a simple and homogenous manner. The fluorescence of the deacetylated reaction product can be analyzed using a plate reader or a fluorometer with excitation wavelengths of 340-360 nm and emission wavelengths of 440-465 nm. An HDAC inhibitor, trichostatin A (TSA), is included for checking specificity of the HDAC reaction. This assay parallels Cayman’s HDAC Activity Assay Kit (Catalog No. 10011563), which uses a nuclear extract rather than whole cells for the assay. Together, both assays will help to identify whether an inhibitor/activator has a direct effect on the enzyme.
|
600150 |
|
| 11-09 |
For immunochemical analysis of TLR8
Antigen:
synthetic peptide from human TLR8 within the region of amino acids 750-850
·
Host:
Mouse
·
Isotype:
IgG1κ
·
Application(s):
WB, FC (intracellular and cell surface), IHC (paraffin-embedded sections)
·
|
13592 |
|
| 11-09 |
For immunochemical analysis of TLR9
Antigen:
human TLR9 amino acids 268-284
·
Clone designation:
26C593.2
·
Host:
Mouse
·
Isotype:
IgG1κ
·
Application(s):
WB, FC (intracellular and cell surface), IHC (frozen and paraffin-embedded sections), and ICC
·
|
13593 |
|
| 11-06 |
A melatonin receptor agonist and 5-HT antagonist
Agomelatine is a metabolically stable analog of melatonin that displays agonist activity for MT1 and MT2 binding with nanomolar affinity. However, unlike melatonin, agomelatine is a competitive antagonist of human and porcine serotonin (5-HT2C) receptors (pKi = 6.2 and 6.4, respectively) as well as human 5-HT2B receptors (pKi = 6.6). Agomelatine abolishes 5-HT2C agonist effects both in cells and in vivo. It also dose-dependently increases extracellular levels of noradrenaline and dopamine in frontal cortex of freely moving rats.
|
13203 |
|
| 11-06 |
A synthetic estrogen
Quinestrol is a synthetic estrogen that is effective in hormone replacement therapy. It is a 3-cyclopentyl ether of ethynyl estradiol. After gastrointestinal absorption, it is stored in adipose tissue, where it is slowly released and metabolized in the liver to its active form, ethinyl estradiol. Quinestrol has found limited use in suppressing lactation in postpartum women and, in combination with synthetic progestogens, as contraceptive therapy, although additional studies are needed for both applications.
|
10006320 |
|
| 11-05 |
Potential metabolite of PGF1α and PGF2α
13,14-dihydro-15-keto tetranor Prostaglandin F1α is a potential metabolite of either PGF1α or PGF2α and likely precursor to tetranor-PGFM
|
13571 |
|
| 11-05 |
For immunochemical detection of Cav1.2
Antigen:
fusion protein amino acids 1,507-1,733
·
Clone designation:
S-57-46
·
Host:
mouse
·
Isotype:
IgG2b
·
Application(s):
WB, IHC, ICC, and IF
·
|
13702 |
|
| 11-05 |
For immunochemical detection of Cav1.3
Antigen:
fusion protein amino acids 2,025-2,161 (C-terminal) of rat Cav1.3
·
Clone designation:
S38-8
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IHC, ICC, and IF
·
|
13703 |
|
| 11-05 |
For immunochemical detection of Cavβ1
Antigen:
synthetic peptide from rat Cavβ4 amino acids 458-474
·
Clone designation:
S10-7
·
Host:
Mouse
·
Isotype:
IgG1
·
Application(s):
WB, IHC, ICC, and IF
·
|
13701 |
|
| 11-05 |
A chemical probe for sulfenic acid detection
DAz-2 is a cell-permeable chemical probe that reacts specifically with sulfenic acid-modified proteins. The azido group of DAz-2 provides a method for selective conjugation to phosphine- or alkynyl- derivatized reagents, such as biotin or various fluorophores, for subsequent analysis of the labeled proteins. Use of DAz-2 in HeLa cells followed by Staudinger ligation to biotin and subsequesnt LC-MS/MS analysis, led to the identification 193 sulfenic acid-modified proteins having a diverse range of functions.
|
13382 |
|
| 11-05 |
A histone deacetylase inhibitor
MS-275 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM). However, it does not inhibit HDAC8 (IC50 > 100 μM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin, inhibitors of poly (ADP-ribose) polymerase (PARP), or inhibitors of heat shock protein 90 (Hsp90).
|
13284 |
|
| 11-04 |
Potent inhibitor of FAAH
4-(n-Nonyl) benzeneboronic acid is a potent inhibitor of FAAH, with an IC50 of 9.1 nM. It is also able to inhibit monoacylglycerol lipase (MAGL), which hydrolyzes 2-arachidonoyl glycerol (2-AG), but at ~1000-fold higher concentration (IC50 = 7.9 μM).
|
13140 |
|
| 11-04 |
Inhibitor of PI3Kγ
CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively). Tested against a panel of 80 other kinases, CAY10505 significantly inhibits only the unrelated casein kinase 2 (CK2, IC50 = 20 nM). It also inhibits the phosphorylation of the PI3K substrate PKB/Akt in murine macrophages (IC50 = 228 nM). Oral administration of CAY10505 reduces neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.
|
10009078 |
|
| 11-03 |
Inhibitor of autotaxin
Palmitoleoyl 3-carbacyclic phosphatidic acid (3-ccPA 16:1) is a cyclic LPA analog that contains the 16:1 fatty acid, palmitoleate, at the sn-1 position of the glycerol backbone. At 25 μM, it inhibits the transcellular migration of MM1 cells across mesothelial cell monolayers in response to fetal bovine serum (86.9%) or LPA (99.9%) without affecting proliferation. 3-ccPA 16:1 significantly inhibits autotaxin (IC50 = 620 nM), an enzyme that is important in cancer cell survival, growth, migration, invasion and metastasis. When delivered intraperitoneally, 3-ccPA 16:1 significantly reduces the number of lung metastases formed in mice injected with B16F10 melanoma cells in the tail vein.
|
10010298 |
|
| 11-01 |
For immunochemical analysis of TLR2
Antigen:
CHO cells transfected with human TLR2 cDNA
·
Clone designation:
TL2.1
·
Host:
murine
·
Isotype:
IgG2a
·
Application(s):
WB, FC (intracellular and cell surface), ICC, IP, and IHC
·
|
13587 |
|
| 11-01 |
For immunochemical analysis of TLR6
Antigen:
synthetic peptide from murine TLR6
·
Host:
rabbit
·
Application(s):
WB and FC (intracellular)
·
|
13590 |
|
| 10-28 |
Potential metabolite of PGD2
13,14-dihydro-15-keto-tetranor PGD2 is a potential metabolite of PGD2. It would be produced from the known metabolite 13,14-dihydro-15-keto PGD2 (Catalog No. 12610), which is a known agonist for the CRTH2/DP2 receptor.
|
13100 |
|
| 10-28 |
Regulator of TetR and revTetR transcriptional repressors
Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet. Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet, so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.
|
10009542 |
|
| 10-28 |
Biotin-tagged FTY720 analog
Biotin-FTY720 is a biotin-tagged analog of FTY720. The hydroxy methyl side chain of FTY720 that is targeted for phosphorylation by sphingosine kinases is retained in this analog, suggesting that it would likewise be phosphorylated in vivo.
|
13254 |
|
| 10-28 |
Inhibitor of protein kinase C
Ro 31-8220 is a potent, cell-permeable bisindolylmaleimide inhibitor of protein kinase C (PKC) isoforms (IC50 = 5, 24, 14, 27, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively). It is a poor inhibitor of protein kinase A (PKA, IC50 = 0.9 μM) and calcium/calmodulin kinase II (IC50 = 17 μM). Ro 31-8220 also inhibits glycogen synthase kinase 3 (IC50 = 6.8 nM).
|
13334 |
|
| 10-27 |
Non-specific inhibitor of cAMP and cGMP phosphodiesterases
IBMX is a widely-used non-specific inhibitor of cyclic AMP and cyclic GMP phosphodiesterases (PDEs) (IC50 = 19, 50, 18, 13, 32, 7, and 50 μM for PDE1, PDE2, PDE3, PDE4, PDE5, PDE7, and PDE11, respectively). PDE8A, PDE8B, and PDE9 are insensitive to IBMX. By inhibiting PDEs, IBMX increases cellular cAMP and cGMP levels, activating cyclic-nucleotide-regulated protein kinases. Methylxanthines, including IBMX, caffeine, and theophylline, bind adenosine receptors, typically antagonizing the suppressive effects of natural agonists.
|
13347 |
|
| 10-27 |
For immunochemical analysis of TLR3
Antigen:
human TLR3 of amino acids 55-70
·
Clone designation:
40C1285.6
·
Host:
mouse
·
Application(s):
WB, FC (intracellular and cell surface), IP, IHC, and ICC
·
|
13588 |
|
| 10-27 |
For immunochemical analysis of TLR4
Antigen:
Ba/F3 cell line expressing human TLR4 cell surface antigen
·
Clone designation:
HTA125
·
Host:
mouse
·
Isotype:
IgG2aκ
·
Application(s):
FC (intracellular and cell surface), IP, neutralization, and ICC
·
|
13589 |
|
| 10-27 |
For immunochemical analysis of TLR5
Antigen:
synthetic peptide corresponding to a portion of human TLR5
·
Clone designation:
85B152.5
·
Host:
mouse
·
Isotype:
IgG2a
·
Application(s):
WB and FC (intracellular and cell surface)
·
|
13595 |
|
| 10-26 |
A competitive assay for the quantification of 8-isoprostane
Limit of detection:
80% B/B0: 10 pg/ml
·
Sensitivity:
50% B/B0: 50 pg/ml
·
Cayman’s 8-Isoprostane Express EIA is a competitive assay that can be used for quantification of 8-isoprostane in plasma, serum, urine, whole blood, tissue culture supernatants, and other sample matrices. The EIA typically displays an IC50 (50% B/B0) of approximately 50 pg/ml and a detection limit (80% B/B0) of approximately 10 pg/ml.
|
516360 |
|
| 10-26 |
For immunochemical detection of NMDA
Antigen:
fusion protein containing amino acids 1-564 of the NR1 subunit of rat NMDA receptor
·
Host:
murine
·
Application(s):
WB and IP
·
|
10607 |
|
| 10-26 |
For immunochemical detection of NMDA
Antigen:
fusion protein from the C-terminus of the NR2A subunit of rat NMDA receptor
·
Host:
rabbit
·
Application(s):
WB, IHC, and IP
·
|
10608 |
|
| 10-26 |
For immunochemical detection of NMDA
Antigen:
fusion protein from the C-terminus of the NR2B subunit of rat NMDA receptor
·
Host:
rabbit
·
Application(s):
WB, IHC, and IP
·
|
10609 |
|
| 10-24 |
For immunochemical detection of Cavβ1
Antigen:
synthetic peptide from rat Cavβ1 amino acids 19-34
·
Clone designation:
S7-18
·
Host:
Mouse
·
Isotype:
IgG2a
·
Application(s):
WB, IHC, and ICC
·
|
13700 |
|
| 10-23 |
Potential metabolite of PGE2
13,14-dihydro-15-keto tetranor PGE2 is a potential metabolite of PGE2. It would be produced from the known metabolite 13,14-dihydro-15-keto PGE2 (Catalog No. 14650), which is known to have a short plasma half-life.
|
13101 |
|
| 10-23 |
Inhibitor of SIRT1
EX-527 is a cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM). It inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs. EX-527 has been used to investigate the relationship between SIRT1-mediated deacetylation of p53, p53 activity, and cell survival following DNA damage.
|
10009798 |
|
| 10-23 |
A tyrosine kinase inhibitor
Nilotinib is a second generation tyrosine kinase inhibitor that is reported to have been used in targeted therapy for cancer. Specifically, it potently inhibits Bcr/Abl tyrosine kinase and is effective in the treatment of chronic myeloid leukemia (MLL) or Philadelphia chromosome acute lymphoblastic leukemia (Ph+ ALL), even in patients who are resistant to the first generation drug, imatinib (Gleevec). Nilotinib is ~20-fold more potent than imatinib in inhibiting both wild-type and mutant Bcr/Abl (e.g., IC50 = 15 versus 280 nM, respectively, for wild-type Bcr/Abl). Also, nilotinib regulates the gene expression for DNA helicase complex, cyclins, and cyclin-dependent kinases, inhibiting cell proliferation and decreasing progression through S phase, while imatinib does not.
|
10010422 |
|
| 10-23 |
For immunochemical detection of Synapsin I
Antigen:
native protein purified from bovine brain
·
Host:
rabbit
·
Application(s):
WB
·
|
10606 |
|
| 10-23 |
For immunochemical detection of Synapsin I
Antigen:
native protein purified from bovine brain
·
Host:
rabbit
·
Application(s):
WB
·
|
10605 |
|
| 10-23 |
For immunochemical detection of Hydroxylase
Antigen:
SDS-denatured rat tyrosine hydroxylase, purified from pheochromocytoma
·
Host:
rabbit
·
Application(s):
WB, IF, and IHC
·
|
10604 |
|
| 10-22 |
Inhibitor of SIRT2
AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels. It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression. AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.
|
13145 |
|
| 10-22 |
For immunochemical detection of DARPP-32
Antigen:
phosphopeptide corresponding to amino acid residues surrounding phospho-Thr34 of rat DARPP-32
·
Host:
rabbit
·
Application(s):
WB
·
|
10603 |
|
| 10-22 |
For immunochemical detection of GABAA
Antigen:
fusion protein from the N-terminus of the δ-subunit of rat GABAA receptor
·
Host:
rabbit
·
Application(s):
WB, IHC, and IP
·
|
10600 |
|
| 10-22 |
For immunochemical detection of GluR1
Antigen:
phosphopeptide corresponding to amino acid residues surrounding the phospho-Ser831 of GluR1
·
Host:
rabbit
·
Application(s):
WB
·
|
10602 |
|
| 10-22 |
For immunochemical detection of GluR1
Antigen:
phosphopeptide corresponding to amino acid residues surrounding the phospho-Ser845 of GluR1
·
Host:
rabbit
·
Application(s):
IHC and WB
·
|
10601 |
|
| 10-22 |
A colorimetric method for screening MGL inhibitors
Cayman’s Monoacylglycerol Lipase (MAGL) Inhibitor Screening Assay provides a convenient method for screening human MAGL inhibitors. MAGL hydrolyzes 4-nitrophenylacetate resulting in a yellow product, 4-nitrophenol, with an absorbance of 405-412 nm.
|
705192 |
|
| 10-21 |
An endothelial lipase inhibitor
GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM). Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
|
13009 |
|
| 10-21 |
Immunosuppressant that blocks mTORC1 signaling
Rapamycin is an immunosuppressant that is used primarily to prevent the rejection of organ and bone marrow transplant. It was first described as a potent inhibitor of IL-2 activation of lymphocytes (IC50 = 5 pM). It is now known that rapamycin specifically interacts with the cytosolic FK-binding protein 12 (FKBP12) to form a complex which inhibits the mammalian target of rapamycin (mTOR) pathway by directly binding to mTOR Complex 1 (mTORC1). Rapamycin and other inhibitors of mTORC1 signaling show potential in treating cancer, adipogenesis, diabetes, tuberous sclerosis, and cardiovascular disease.
|
13346 |
|
| 10-21 |
HDAC inhibitor with numerous in vivo applications
Valproic acid is an analog of the natural fatty acid valeric acid. The sodium salt of valproic acid has long been used as an anticonvulsant to prevent many kinds of seizures. It is an inhibitor of histone deacetylases (HDACs), inhibiting Class I HDACs with an IC50 of ~ 2 mM. Valproic acid also inhibits glycogen synthase kinase (GSK3) and depletes cellular inositol-1,4,5-trisphosphate (IP3). Because of these actions, valproic acid shows promise in combination therapy for cancer and in treating Alzheimer’s disease. Valproic acid (1 mM) also has pronounced effects on stem cell differentiation and self-renewal.
|
13033 |
|
| 10-15 |
Potent antagonist of the thromboxane A2 receptor
L-655,240 is a potent antagonist of the TP receptor in vitro (IC50 = 7 nM). It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo. Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known.
|
10011562 |
|
| 10-14 |
Inhibitor of H2O2-induced necrotic cell death
IM-54 is an indolylmaleimide derivative which, at 1 μM, inhibits necrotic cell death induced by H2O2 in promyelocytic leukemia HL-60 cells. It does not prevent etoposide-induced apoptosis and does not inhibit protein kinase C or S6 kinase 1.
|
13323 |
|
| 10-14 |
Inhibitor of autotaxin, antagonist of LPA1 and LPA3
Oleoyl 3-carbacyclic phosphatidic acid (3-ccPA 18:1) is a cyclic LPA analog that contains the 18:1 fatty acid, oleate, at the sn-1 position of the glycerol backbone. At 25 μM, it inhibits the transcellular migration of MM1 cells across mesothelial cell monolayers in response to fetal bovine serum (90.1%) or LPA (99.9%) without affecting proliferation. 3-ccPA 18:1, at 0.1-1.0 μM, significantly inhibits autotaxin, an enzyme that is important in cancer cell survival, growth, migration, invasion, and metastasis.
|
10010299 |
|
| 10-12 |
An analog of PGF2α
16-phenoxy tetranor prostaglandin F2α cyclopropyl methyl amide (16-phenoxy tetranor PGF2α cyclopropyl methyl amide) is an analog of PGF2α containing a 16-phenoxy group on the lower (ω) side chain and a cyclopropyl methyl amide at the C-1 position. There are no published reports on the biological activity of 16-phenoxy tetranor PGF2α cyclopropyl methyl amide.
|
10010809 |
|
| 10-12 |
For immunochemical analysis of eIF3G
Antigen:
synthetic peptide from human eIF3G within the region of amino acids 200-250
·
Host:
rabbit
·
Application(s):
WB and IHC (paraffin-embedded sections)
·
|
13537 |
|
| 10-10 |
For immunochemical analysis of TLR1
Antigen:
synthetic peptide from human TLR1 amino acids 400-450
·
Host:
rabbit
·
Application(s):
WB and FC (intracellular and cell surface)
·
|
13582 |
|
| 10-08 |
Inhibitor of sphingosine-1-phosphate lyase
2-Acetyl-5-tetrahydroxybutyl imidazole (THI) is an inhibitor of S1P lyase. Because S1P lyase is primarily expressed in lymphatic tissue, treatment of mice with THI (50 µg/ml in drinking water) increases lymphoid tissue S1P concentrations 100-fold, reducing lymphocyte egress from thymus and peripheral lymphoid organs. The resulting lymphopenia is reversible following cessation of THI treatment. Reducing S1P lyase activity results in therapeutic levels of immunosuppression without the non-lymphoid lesions that result from synthetic S1P receptor agonists.
|
13222 |
|
| 10-07 |
A selective inhibitor of MMP-2
CAY10609 is a biphenylsulfonamide that acts as a selective inhibitor of MMP-2 demonstrating an IC50 value of 12 nM. Due to its specific zinc binding domain configuration, the inhibitory activity of CAY10609 is significantly less potent towards MMP-1, MMP-3, MMP-7, and MMP-9 (IC50 values are 50, 4.5, 50, and 2 µM, respectively). At 50 nM, CAY10609 suppresses the invasive behavior of HT1080 tumor cells grown on matrigel.
|
13321 |
|
| 10-07 |
Inhibitor of protein kinase C
Gö 6983 inhibits several isoforms of protein kinase C (PKC; IC50 = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively). It provides cardioprotective effects in myocardial ischemia/reperfusion by attenuating contractile dysfunction.
|
13311 |
|
| 10-07 |
N-Desethylamiodarone hydrochloride is a CYP3A4 metabolite of amiodarone
|
9000537 |
|
| 10-07 |
Inhibitor of autotaxin
Palmitoyl 3-ccPA is a cyclic LPA analog that contains the 16:0 fatty acid, palmitate, at the sn-1 position of the glycerol backbone. At 25 μM, it inhibits the transcellular migration of MM1 cells across mesothelial cell monolayers in response to fetal bovine serum (81.9%) or LPA (98.9%) without affecting proliferation. 3-ccPA 16:0, at 0.1-25 μM, significantly inhibits autotaxin, an enzyme that is important in cancer cell survival, growth, migration, invasion and metastasis.
|
10010293 |
|
| 10-07 |
Inducer of autophagy in renal cell carcinoma cells
STF-62247 is a small molecule agonist that induces autophagy and selectively causes lethality in renal cell carcinoma (RCC) cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 nM). It significantly reduces the growth rate of tumors formed from VHL-deficient cells in mice. STF-62247 induces cytotoxicity in VHL-positive RCC cells only at higher concentrations (IC50 = 16 μM).
|
13084 |
|
| 10-01 |
A commonly used anti-coagulant
(−)-Warfarin differs from (+)-warfarin by being five times more potent as a vitamin K antagonist. However, the two isomers are metabolized in vivo by different pathways, and (−)-warfarin has a shorter terminal elimination half-life (24-33 hours) than (+)-warfarin (35-58 hours).
|
13531 |
|
| 10-01 |
A commonly used anti-coagulant
(+)-Warfarin differs from (−)-warfarin by being five times less potent as a vitamin K antagonist. However, the two isomers are metabolized in vivo by different pathways, and (+)-warfarin has a longer terminal elimination half-life (35-58 hours) than (−)-warfarin (24-33 hours).
|
13526 |
|
| 09-30 |
For immunochemical analysis of DNA methyltransferase 1-associated protein 1
Antigen:
synthetic peptide from human DMAP1 within the region of amino acids 250-300
·
Host:
rabbit
·
Application(s):
WB and IHC (paraffin-embedded sections)
·
|
13536 |
|
| 09-30 |
For immunochemical analysis of eIF4B
Antigen:
synthetic peptide from human eIF4B within the region of amino acids 570-630
·
Host:
rabbit
·
Application(s):
WB
·
|
13529 |
|
| 09-30 |
Internal standard for the quantification of GW 9662
GW 9662-d5 contains five deuterium atoms at the 10, 11, 12, 13, and 14 positions. It is intended for use as an internal standard for the quantification of GW 9662 by GC- or LC-mass spectrometry.
|
9000497 |
|
| 09-30 |
A tight-binding inhibitor of class I HDACs
Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases (HDACs). Unlike the HDAC inhibitor suberoylanilide hydroamic acid, which has a fast-on/fast-off HDAC binding rate, pimelic diphenylamide 106 progressively binds HDACs and remains bound after wash-out. As a result, the IC50 of pimelic diphenylamide 106 decreases over time. With prolonged preincubation (1-3 hours), pimelic diphenylamide inhibits the class I HDACs (IC50 = 150, 760, 370, and 5,000 nM for HDAC1, 2, 3, and 8, respectively) but not the class II HDACs (IC50 > 180 μM for HDAC4, 5, and 7). Pimelic diphenylamide 106 and related benzamide HDAC inhibitors may have therapeutic value in Friedrich’s ataxia and Huntington’s disease, in part due to their low animal toxicity.
|
13212 |
|
| 09-29 |
A commonly used anti-coagulant
(±)-Warfarin is a racemic mixture of two optically active isomers. (±)-Warfarin has a half-life of 36-42 hours in circulation, bound to plasma proteins, and accumulates in the liver, where the two isomers are metabolized by different pathways. Genetic differences in metabolic enzymes, drugs, diet, and disease state can affect the clearance, and thus the response, to warfarin. As a result, levels of the two enantiomers must be monitored carefully. (±)-Warfarin is also used as a rodenticide.
|
13566 |
|
| 09-25 |
Activator of γδ-T-lymphocytes
(E)-C-HDMAPP is the pyrophosphonate form of (E)-HDMAPP. The pyrophosphonate moiety in (E)-C-HDMAPP is much less susceptible to chemical or enzymatic hydrolysis than its pyrophosphate counterpart. As a result, (E)-C-HDMAPP is much more stable in solution and in vascular circulation. (E)-C-HDMAPP possesses comparable activity to (E)-HDMAPP, which is the most potent of the isoprenoid phosphoantigens. (E)-C-HDMAPP stimulates the synthesis of tumor necrosis factor (TNF-α) by γδ-T lymphocytes with an IC50 value of 0.91 nM. (E)-C-HDMAPP also significantly increases the number of circulating γδ-T cells in vivo, in cynomolgus monkeys.
|
13151 |
|
| 09-23 |
Isomer of bimatoprost
5-trans Bimatoprost is an isomer of bimatoprost wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of bimatoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity of 5-trans bimatoprost.
|
10008132 |
|
| 09-23 |
6α-hydroxy Paclitaxel is a CYP2C8 metabolite of paclitaxel.
|
19027 |
|
| 09-22 |
A synthetic intermediate useful for pharmaceutical synthesis
2-methyl-4-phenyl Thiazole is a synthetic intermediate useful for pharmaceutical synthesis.
|
13386 |
|
| 09-22 |
For immunochemical analysis of ARRB2
Antigen:
synthetic peptide from human ARRB2 within the region of amino acids 15-50
·
Host:
rabbit
·
Application(s):
WB and IHC
·
|
13498 |
|
| 09-22 |
For immunochemical analysis of Brd4/HUNK1
Antigen:
synthetic peptide from human Brd4 within the region of amino acids 150-200
·
Host:
rabbit
·
Application(s):
WB
·
|
13497 |
|
| 09-22 |
For immunochemical analysis of CAP-C
Antigen:
synthetic peptide from human CAP-C amino acids 281-297
·
Host:
rabbit
·
Application(s):
WB
·
|
13501 |
|
| 09-22 |
For immunochemical analysis of CAP-C
Antigen:
synthetic peptide from human CAP-C amino acids 47-61
·
Host:
rabbit
·
Application(s):
WB
·
|
13503 |
|
| 09-22 |
A synthetic intermediate useful for pharmaceutical synthesis
ethyl-2-amino-4-phenyl-Thiophene-3-carboxylate is a synthetic intermediate useful for pharmaceutical synthesis.
|
13387 |
|
| 09-21 |
Inhibitor of DNA-dependent protein kinase
NU 7026 is a cell-permeable, potent, specific, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM). It poorly inhibits phosphioinositide 3 kinase (IC50 = 13 μM) and is inactive against ataxia telangiectasia mutated kinase, ATR, and poly (ADP-ribose) polymerase. NU 7026 impairs cellular DNA double strand break repair and decreases survival in cells exposed to ionizing radiation. It also potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia. For example, it potentiates the growth inhibitory effects of mitoxantrone in K562 cells more than 10-fold.
|
13308 |
|
| 09-18 |
A soluble adenylyl cyclase inhibitor
KH7 is a selective inhibitor of soluble adenylyl cyclase (sAC) that has little effect on transmembrane adenylyl cyclases. It displays an IC50 value between 3-10 µM toward sAC. At 50 µM, KH7 decreases basal cAMP accumulation in sperm. KH7 has been used in diverse research applications including cAMP-mediated signaling events required for mammalian egg fertilization, sAC regulation of Na+ transport in the kidney, and mitochondrial-dependent apoptosis in response to various stress stimuli.
|
13243 |
|
| 09-18 |
A potent inhibitor of phosphatidic acid generation
(±)-Lisofylline (LSF), a unique metabolite of pentoxifylline, is a potent inhibitor of phosphatidic acid formation (IC50 = 0.6 µM) through cytokine-activated lysophosphatidic acyl transferase (LPAAT) that has been shown to protect mice from endotoxic shock. LSF suppresses the production of the proinflammatory cytokine interferon-γ, inhibits interleukin-12-mediated STAT-4 activation and enhances glucose-stimulated β-cell insulin secretion, reducing the onset of diabetes in a non-obese diabetic murine model.
|
10010785 |
|
| 09-14 |
A synthetic intermediate useful for pharmaceutical synthesis
5-(2-Aminopyridyl)amide oxime is a synthetic intermediate useful for pharmaceutical synthesis.
|
13384 |
|
| 09-14 |
Isomer of D-myo-inositol-1,4,5-triphosphate
Ins(1,4,5)P3 is an isomer of the biologically important D-myo-inositol-1,4,5-triphosphate. Unlike its isomer, Ins(1,4,5)P3 does not evoke a rise in intracellular calcium when added to cells. It is not known if Ins(1,4,5)P3 can act as a competitive inhibitor of biologically-active inositol phosphates.
|
10008426 |
|
| 09-09 |
For immunochemical analysis of Bnc 1
Antigen:
synthetic peptide from human Bnc 1 within the region of amino acids 330-380
·
Host:
rabbit
·
Application(s):
WB
·
|
13502 |
|
| 09-09 |
Natural resveratrol analog
Pterostilbene is a naturally-occurring dimethyl ether analog of resveratrol that is abundant in blueberries. Like resveratrol, pterostilbene acts as a powerful antioxidant, suppresses the synthesis of prostaglandin E2 from lipopolysaccharide-stimulated human peripheral blood mononuclear cells (IC50 = 1.0 μM for pterostilbene, 3.2 μM for resveratrol), and inhibits cell proliferation (IC50 ~60 μM for both compounds). Pterostilbene blocks the activation of ERK1/2, p38 MAPK, and PI3K/Akt signaling pathways, reducing NF-κB and AP-1 transcriptional activation. Through these actions, pterostilbene evokes effects that prevent cancer, inflammation, and diabetes.
|
13000 |
|
| 09-08 |
A water soluble p38 MAPK inhibitor
SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580.
|
13344 |
|
| 09-03 |
For immunochemical analysis of ARAP2
Antigen:
synthetic peptide from human ARAP2 within the region of amino acids 1,670-1,720
·
Host:
rabbit
·
Application(s):
WB and IHC
·
|
13495 |
|
| 09-03 |
For immunochemical analysis of AROS
Antigen:
synthetic peptide from human AROS within the region of amino acids 1-50
·
Host:
rabbit
·
Application(s):
WB
·
|
13496 |
|
| 09-03 |
Selective inhibitor of phospholipase D1
CAY10593 is a potent and selective inhibitor of phospholipase D (PLD)1, both in vitro (IC50 = 46 nM) and in cells (IC50 = 11 nM). It is also effective as a PLD2 inhibitor at higher concentrations (IC50 = 933 nM in vitro, 1,800 nM in cells). CAY10593 strongly inhibits the invasive migration of several breast cancer cell lines in transwell assays, suggesting that PLD might be a useful target in blocking tumor cell invasion.
|
13206 |
|
| 09-03 |
An estrogen receptor agonist
Equol is a nonsteroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzein by human intestinal microflora. The estrogen receptor (ER) binding activity of the naturally occurring (S)-enantiomer demonstrates greater affinity toward ERβ while the (R)-enantiomer demonstrates greater affinity towards ERα. Synthesized as a racemic mixture, (±)-equol exhibits EC50 values of 200 and 74 nM for human ERα and ERβ, respectively and induces breast cancer cell proliferation in vitro at concentrations as low as 100 nM.
|
13184 |
|
| 09-03 |
HDAC inhibitor
HNHA is a cell-permeable inhibitor of histone deacetylase (HDAC) activity (IC50 = 100 nM). In human fibrosarcoma HT1080 cells, it induces histone hyperacetylation and p21 transcription with concomitant inhibition of cell cycle progression (IC50 ~ 7.5 μM). HNHA is at least as effective as SAHA in inhibiting tumor growth in a murine xenograph model in vivo. HNHA also blocks the growth of human umbilical vein endothelial cells (HUVECs) and prevents tube formation and migration of HUVECs in response to vascular endothelial growth factor (VEGF). It also blocks retinal neovascularization and choroidal angiogenesis in mice.
|
13295 |
|
| 09-03 |
Hydrogen sulfide (H2S) donor
Sodium hydrogen sulfide is an hydrogen sulfide (H2S) donor commonly used in cellular and whole animal experimental systems. For example, it has been used to suggest that H2S promotes neutrophil migration, reduces airway inflammation, and protects neurites, heart, and intestine from chemical or ischemic-reperfusion damage.
|
10012555 |
|
| 08-28 |
A PKC inhibitor
Bisindolylmaleimide I (BIM) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine. It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα-, β1-, β2-, γ-, δ-, and ε-isozymes. BIM directly inhibits GSK3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM). This compound also competitively antagonizes the 5-HT3 receptor with a Ki value of 61 nM.
|
13298 |
|
| 08-28 |
Inhibitor if MAPK-interacting kinase1
CGP 57380 is a selective inhibitor of MAP kinase-interacting kinase 1 (MNK1) in vitro (IC50 = 2.2 μM), with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases. It blocks the phosphorylation of eIF4E in response to TNF-α, arsenite, anisomycin, PMA, or fetal calf serum in 293 cells (IC50 = 3 μM). CGP 57380 also dose-dependently inhibits TNF-α production in RAW 264.7 cells that have been co-treated with agonists for Toll-like receptor (TLR)2 (HKLM), TLR4 (LPS), TLR6/2 (FSL), TLR7 (imiquimod), or TLR9 (CpG DNA), presumably by inhibiting MNK1.
|
13322 |
|
| 08-27 |
For immunochemical analysis of androgen receptor
Antigen:
synthetic peptide from human androgen receptor amino acids 207-221
·
Clone designation:
156C135.2
·
Host:
Mouse
·
Application(s):
WB and IHC (paraffin-embedded)
·
|
13492 |
|
