| 03-17 |
A selective sEH inhibitor
N,N’ Dicyclohexylurea (DCU) is a selective sEH inhibitor with IC50 values of 160 and 90 nM for recombinant human and murine sEH, respectively. At 10 µM, DCU blocks the hydrolysis of cis- and trans-EETs by rat red blood cells and porcine coronary endothelial cells as well as completely inhibits 14,(15)-EET-induced PPARα activation.
|
10004971 |
|
| 03-16 |
A plant hormone with diverse roles
Abscisic acid (ABA) is a plant hormone with diverse roles in disease resistance, plant development, and response to stresses (water, salt, temperature, and pathogens). It is also produced by some plant pathogenic fungi. In addition to key roles in regulating stomatal closing, seed dormancy, and cell division, ABA regulates gene expression and may contribute to epigenetic changes at the chromatin level. The (+)-enantiomer is the naturally occurring and more active form of ABA.
|
10073 |
|
| 03-16 |
A His-tagged protein for Hsp research
Source:
recombinant N-terminal hexahistadine-tagged protein, expressed in E. coli
·
Mr:
87 kDa
·
|
10202 |
|
| 03-16 |
A His-tagged protein for Hsp research
Source:
recombinant N-terminal hexahistadine-tagged protein, expressed in E. coli
·
Mr:
85.6 kDa
·
|
10342 |
|
| 03-10 |
For immunochemical detection of AdPLA2
Antigen:
human AdPLA2 amino acids 147-162 (MSLIGVMFSRNKRQKQ)
·
Host:
rabbit
·
Application(s):
WB
·
|
10337 |
|
| 03-10 |
A selective p110α inhibitor
PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM. It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively. In adipocytes and myotubes, PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1.
|
10009210 |
|
| 03-10 |
A selective S1P1 receptor antagonist
W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material). No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.
|
10009109 |
|
| 03-09 |
A selective EP1 antagonist
SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a murine writhing assay with an ED50 value of 0.9 mg/kg. It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089. SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.
|
10010744 |
|
| 03-09 |
A convenient method for screening human SET8 inhibitors
Cayman’s SET8 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET8 inhibitors. The transfer of the methyl group from SAM by SET8 to the acceptor peptide (H4K20) 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 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) 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.
|
700350 |
|
| 03-09 |
Save time and money with Columbia Bioscience’s Western blot detection kits. SureLight® Western kits provide the same sensitivity as enzymatic chemiluminescence (ECL) and enzymatic chemifluorescence (ECF) reagents. These assays are up to 16X more sensitive than other fluorescent kits. So, you can loose the enzyme and save up to an hour in processing your blots but keep the sensitivity. The Western Kit (P112) features sensitive fluorescent detection with a Goat Anti-Mouse SureLight® P3 conjugate. Sufficient buffers and detection reagent are provided for up to ten 10 x 10 cm2 blots.
|
13749 |
|
| 03-09 |
Save time and money with Columbia Bioscience’s Western blot detection kits. SureLight® Western kits provide the same sensitivity as enzymatic chemiluminescence (ECL) and enzymatic chemifluorescence (ECF) reagents. These assays are up to 16X more sensitive than other fluorescent kits. So, you can loose the enzyme and save up to an hour in processing your blots but keep the sensitivity. The Western Kit (P114) features sensitive fluorescent detection with a Goat Anti-Rabbit SureLight® P3 conjugate. Sufficient buffers and detection reagent are provided for up to ten 10 x 10 cm2 blots.
|
13767 |
|
| 03-08 |
A synthetic intermediate useful for pharmaceutical synthesis
2-amino-4-phenyl Thiazole is a synthetic intermediate useful for pharmaceutical synthesis.
|
13388 |
|
| 03-08 |
AChE inhibitor used to treat Alzheimer’s disease
Donepezil is a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine. It has a half-life in circulation of about 70 hours. As acetylcholine modulates plasticity, excitability, and arousal in the central nervous system, donepezil is commonly used in the treatment of Alzheimer’s disease to improve cognition, memory, and behavior. In this way, it is intended to prevent or reverse dementia. Studies on these effects have been equivocal, indicating that more research into the therapeutic potential of donepezil is warranted.
|
13245 |
|
| 03-08 |
Potent, selective inhibitor of monoacylglycerol lipase
Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC50 = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 µM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).
|
13621 |
|
| 03-08 |
Antigen:
human recombinant SET7/9 (amino acids 1-366)
·
Host:
rabbit
·
Application(s):
WB
·
|
13780 |
|
| 03-04 |
A novel method to assess CYP3A4 induction
Cayman’s CYP3A4 Induction STEP™ Reporter Assay Kit (Luminescence) consists of a 96-well plate coated with a STEP™ complex containing a Secreted Alkaline Phosphatase (SEAP) reporter regulated by the human CYP3A4 gene promoter. The complex also contains two nuclear expression constructs, Pregnane X Receptor (PXR) and Hepatocyte Nuclear Factor-4α (HNF-4α). Cells grown on the CYP3A4 STEP™ Plate will introduce the reporter gene and express the PXR and HNF4 factors. Binding of inducer-activated transcription factors to the CYP3A4 promoter initiates a signal resulting in expression of SEAP, which is secreted into the cell culture medium. Aliquots of medium are removed at time intervals beginning at about 24 hours and SEAP activity is measured simply by adding a luminescence-based alkaline phosphatase substrate provided in the kit. The kit is simple to use and can be easily adapted to high-throughput screening for potential CYP3A4 inducers. A known CYYP3A4 inducer, rifampicin, 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 white plates provided.
|
600270 |
|
| 03-04 |
An internal standard for the quantification of PEA
An internal standard for the quantification of rosiglitazone by GC- or LC-MS
|
9000573 |
|
| 03-03 |
Antigen:
recombinant adenovirus expressing full-length mouse CD36
·
Host:
CD36 null mouse (clone JC63.1)
·
Application(s):
ICC, FC, and functional blocking
·
|
10009893 |
|
| 03-01 |
A competitive assay for the quantification of corticosterone in plasma and fecal samples
Limit of detection:
80% B/B0: 30 pg/ml
·
Sensitivity:
50% B/B0: 150 pg/ml
·
Cayman’s Corticosterone EIA Kit is a competitive assay that can be used for quantification of corticosterone in plasma and fecal samples.
|
500655 |
|
| 03-01 |
Application(s):
enzyme kinetics, inhibitor screening, and selectivity profiling
·
Source:
N-terminal GST-tagged protein from baculovirus expression system
·
Mr:
75.2 kDa
·
|
10009652 |
|
| 02-25 |
Rho kinase inhibitor
H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM). H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 μM, respectively). It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly, vasoconstriction, as well as spontaneously tonic smooth muscle and neurite extension.
|
10007653 |
|
| 02-25 |
An inactive enantiomer of W146
W140 (trifluoroacetate salt) is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 µM (2a = W146; 2b = W140 in supplemental material). It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.
|
10009110 |
|
| 02-19 |
An antithrombic compound
Aspalatone is an anti-platelet aggregator (IC50 = 180 µM, in vitro) that prolongs bleeding time significantly in a rodent model of thromboembolism. Additionally at a minimal effective dose of 24 mg/kg, aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in rat hippocampus.
|
13644 |
|
| 02-19 |
Source:
Recombinant protein expressed in E. coli
·
Mr:
44.5 kDa
·
|
10329 |
|
| 02-19 |
Neuroprotective drug
Dimebolin (hydrochloride), also known as 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 disease and Huntington’s disease. In addition to preventing the onset and progression of disease by being neuroprotective, Dimebolin appears to promote clinical improvement by increasing cognitive function. At the cellular level, Dimebolin 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. The hydrochloride form of Dimebolin is soluble in both aqueous and organic solvents.
|
10011349 |
|
| 02-19 |
A peptide inhibitor of NF-κB p65 phosphorylation
NF-κB has been shown to regulate the expression of a number of genes whose products are involved in inflammation, viral replication, carcinogenesis, antiapoptosis, invasion, and metastasis. Specific adhesion molecules, chemokines, inflammatory cytokines, and cell cycle regulatory genes are affected. Thus, agents that can suppress NF-κB activation have the potential to be treatments for inflammatory diseases and cancer. The Ser276 site of p65 is phosphorylated during NF-kB activation, allowing p65 nuclear translocation. This p65 inhibitory peptide contains a Ser276 site that is phosphorylated during NF-κB activation, thereby blocking p65 Ser276 phosphorylation. The NF-kB (p65) (Ser276) inhibitory peptide, also known as PTD-p65-P1, 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.
|
13758 |
|
| 02-19 |
A peptide inhibitor of NF-κB p65 phosphorylation
NF-κB has been shown to regulate the expression of a number of genes whose products are involved in inflammation, viral replication, carcinogenesis, apoptosis, invasion, and metastasis. Specific adhesion molecules, chemokines, inflammatory cytokines, and cell cycle regulatory genes are affected. Thus, agents that can suppress NF-κB activation have the potential to be treatments for inflammatory diseases and cancer. The Ser529,536 sites of p65 are phosphorylated during NF-κB activation, allowing p65 nuclear translocation. This p65 inhibitory peptide contains the Ser529,536 sites that are phosphorylated during NF-κB activation, thereby blocking p65 phospho-Ser529,536 phosphorylation. The NF-κB (p65) (phospho-Ser529,536) inhibitor peptide can inhibit binding of recombinant p65 protein to DNA in a dose-dependent manner with maximum inhibition occuring at 50 µM. It can also inhibit TNF-induced NF-κB activation in cells. The NF-κB (p65) (Ser529,536) inhibitory peptide also contains a protein transduction (PTD) sequence (DRQIKIWFQNRRMKWKK) derived from antennapedia which renders the peptide cell permable. The control peptide consists of only the PTD sequence.
|
13759 |
|
| 02-18 |
A biotinylating reagent
Biotin-XX hydrazide is a biotylating reagent for carbohydrates and carbonyl compounds that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.
|
13304 |
|
| 02-18 |
For fluorescent analysis of SIRT6
Cayman’s SIRT6 Direct Fluorescent Screening Assay provides a convenient fluorescence-based method for screening SIRT6 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 Arg-His-Lys-Lys(ε-acetyl)-AMC, is incubated with human recombinant SIRT6 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 easily analyzed using an excitation wavelength of 350-360 nm and emission wavelength of 450-465 nm.
|
700290 |
|
| 02-17 |
A plant growth regulator
trans-Zeatin is a member of the plant hormone family known as ‘cytokinins’, which regulate cell division, development, and nutrient processing. The biosynthesis of cytokinins involves isoprenylation of ATP or ADP, with trans-Zeatin being produced by the removal of phosphate and riboside groups from adenine and oxidation by cytochrome P735A. trans-Zeatin evokes its effects through high affinity receptors, including Arabidopsis histidine kinases (AHK). The affinity of trans-zeatin for AHK3, which is important in mediating plant development, has been reported to be 1.3 nM.
|
13226 |
|
| 02-16 |
Selective inhibitor of sphingosine kinase 1
CAY10261 is a selective inhibitor of SphK1, both in vitro (IC50 = 3.3 μM) and in U937 cells overexpressing human SphK1 (70 % inhibition at 5 μM). It has no inhibitory effect on SphK2 either in vitro or in cells. Similarly, CAY10261 does not reduce the activity of protein kinase C (PKC) except at very high concentration (>75 μM).
|
13371 |
|
| 02-16 |
An antimycotic agent that inhibits squalene epoxidase
Terbinafine is an antifungal compound that is highly active against dermatophytes, mold, other basic fungi, and some strains of yeast. It is clinically used to treat nail and skin infections, inhibiting ergosterol synthesis at the stage of squalene epoxidation (IC50 = 30 nM for Candida albicans). At 90-120 µM, terbinafine exhibits antitumor and antiangiogenic activity by inducing cell cycle arrest at the G0/G1 stage in COLO 205 tumor cells and human vascular endothelial cells.
|
10011619 |
|
| 02-15 |
Source:
Recombinant N-terminal His-tagged GRFT, purified from E. coli
·
Mr:
14.6 kDa
·
|
10340 |
|
| 02-15 |
cPLA2 inhibitor
RSC-3388 is a pyrrolidine derivative that acts as a potent inhibitor of cPLA2α, suppressing both recombinant human cPLA2 in vitro (IC50 = 1.8 nM) and cellular PLA2 activity in cells stimulated with the calcium ionophore A23187 (IC50 = 22 nM). In the human acute monocytic leukemia cell line THP-1, RSC-3388 blocks the production of prostaglandin E2 (IC50 = 31 nM) and leukotriene C4 (IC50 = 13 nM). RSC-3388 also reduces skin inflammation in mouse models of atopic dermatitis, presumably through its inhibitory effects on cPLA2.
|
13343 |
|
| 02-12 |
A synthetic intermediate useful for pharmaceutical synthesis
2-amino Pyridyl-5-thioamide is a synthetic intermediate useful for pharmaceutical synthesis.
|
13389 |
|
| 02-12 |
A histone acetyltransferase inhibitor
Anacardic acid, isolated from cashew shells or several other medicinal plants, is the general name given to a family of four different 6-alkyl salicyclic acids having varying degrees of unsaturation in the 15-carbon alkyl chain. These compounds are associated with anti-inflammatory, anti-tumor, molluscicidal, and anti-microbial activity. Literature frequently sites and gives the name anacardic acid to the completely-saturated compound (6-pentadecyl salicylic acid). Anacardic acid inhibits the histone acetyltransferase (HAT) activity of the transcription co-activators p300 and p300/CREB-binding protein-associated factor (pCAF) with IC50 values of 8.5 and 5 µM, respectively. At 25 µmol/L, anacardic acid suppresses NF-κB activation, inhibits IκB-α phosphorylation, and prohibits p65 nuclear translocation in KBM-5 cells.
|
13144 |
|
| 02-12 |
An internal standard for quantification of arachidonic acid methyl ester by GC- or LC-MS
|
390014 |
|
| 02-11 |
An herbicide
Atrazine is an herbicide that is effective in controlling a broad range of weeds. Atrazine has been reported to cause cancer in certain laboratory animals, have diverse effects on the reproductive system in animals and humans, and disrupt the normal function of the endocrine system. Chronic exposure of frogs to atrazine significantly alters the expression of several genes, especially those involved in growth and metabolism. The United States Environmental Protection Agency currently allows the use of atrazine as an herbicide but, in 2009, launched a comprehensive new evaluation to determine its effects on humans.
|
13375 |
|
| 02-11 |
A PDE5 inhibitor
Icariin, the active component of the Chinese medicinal plant E. brevicornum, is an inhibitor of human recombinant PDE5 with an IC50 value of 5.9 µM. It is a prenylated flavonol that has been used to treat erectile dysfunction and has been shown to have anti-cancer and antioxidant activity. At a concentration of 1 x 107 mol/L, icariin induces differentiation of cardiomyocytes and upregulates the expression of cardiac genes. At 20 µg/ml, icariin increases the proliferation and differentiation of cultured human osteoblasts, which appears to be mediated in part by upregulating bone morphogenetic protein 2 mRNA.
|
13624 |
|
| 02-11 |
An EGFR inhibitor
Iressa is a selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50s ranging between 0.2 - 0.4 µM. By interfering with the intracellular kinase domain, iressa prevents EGFR autophosphorylation and prevents downstream signal transduction. Iressa has been used to treat advanced (or recurrent) non-small cell lung cancer (NSCLC). However, the FDA retracted its general approval for this compound when a phase III trial failed to demonstrate an overall survival benefit. Iressa appears to be most efficacious in treating certain EGFR gene mutations that are prevalent in Asian populations.
|
13166 |
|
