| 11-21 |
Inhibitor of 6-phosphogluconate dehydrogenase
6-Aminonicotinamide (6-AN) is a well-established inhibitor of the NADP+-dependent enzyme, 6-phosphogluconate dehydrogenase (Ki = 0.46 μM). Through this action, 6-AN interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, like cisplatin, in killing cancer cells (IC50 = 0.5 mM). 6-AN also reduces cardiovascular oxidative injury following ischemia/reperfusion. In addition, 6-AN causes glial neurodegeneration.
|
10009315 |
|
| 11-21 |
Inhibitor of glucosylceramide synthase and non-lysosomal glucosylceramidase
AMP-deoxynojirimycin (AMP-dNM) is a hydrophobic derivative of dNM. It potently inhibits BGD (IC50 = 0.3 nM), less potently antagonizes GCS (IC50 = 25 nM), but only poorly inhibits other GCase isoforms. AMP-dNM has been shown to strongly suppress inflammation in a murine model of hapten-induced colitis, enhance insulin sensitivity in murine and rat models of insulin resistance, and induce sterol regulatory element-binding protein-regulated gene expression and cholesterol synthesis in HepG2 cells.
|
10010332 |
|
| 11-21 |
A lipid component of CNS gangliosides
Sphingosines are long-chain base precursors of cellular sphingolipids used directly in the synthesis of ceramide, which in combination with sialic acid forms ganglioside. Sphingosine can exist in four stereoisomers, however only D-erythro-sphingosine occurs naturally. Compared to other sphingolipids throughout the body, which are predominantly composed of C-18 sphingosine, only central nervous system (CNS) gangliosides contain significant amounts of D-erythro-sphingosine C-20. The concentration of D-erythro-sphingosine C-20 within mammalian brain gangliosides apparently increases with developmental maturation. Furthermore, the ratio of C-18 to C-20 sphingosine in the brain is thought to be related to some nervous system degeneration processes.
|
10007903 |
|
| 11-21 |
Novel ω-6 dienoic PUFA
Eicosadienoic acid (5Z,14Z) is a novel ω-6 C20:2 fatty acid. The more common eicosadienoic acid (11Z,14Z) competitively inhibits inosine 5’-monophosphate dehydrogenase (Ki = 3.1 µM) and inhibits the binding of LTB4 to its receptor on neutrophils (Ki = 3.0 µM). Also, serum levels of eicosadienoic acids negatively correlate with degree of sleep disturbance. Eicosadienoic acids are converted by desaturases, in vivo, to eicosatrienoic acids, which are potent vasodilators. The physiological effects of eicosadienoic acid (5Z,14Z) are unstudied.
|
10010484 |
|
| 11-21 |
Female mating pheromone of D. melanogaster
7(Z),11(Z)-Heptacosadiene is the predominant female-specific courtship pheromone of the fruit fly D. melanogaster. At concentrations above 100 ng, 7(Z),11(Z)-heptacosadiene elicits wing vibrations in male D. melanogaster flies in a dose-dependent manner.
|
10012567 |
|
| 11-21 |
An antibacterial imidazole
NH125 is an imidazole that has potent antibacterial properties in drug-resistant bacteria . In bacteria, NH125 inhibits several histidine kinases, inhibiting YycG with an IC50 of 6.6 µM . NH125 also decreases the viability of several cancer cell lines with IC50 values ranging from 0.7-4.7 µM . In mammalian cells, NH125 strongly inhibits eEF-2K (IC50 = 60 nM), with weaker effects on protein kinase C (IC50 = 7.5 µM), protein kinase A (IC50 = 80 µM), and calmodulin-dependent kinase II (IC50 = 100 µM).
|
10011250 |
|
| 11-17 |
A positional isomer of LXA4
LXB4 is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15-HpETE by human leukocytes. At a concentration of 10-7 M, LXB4 inhibits PMN migration stimulated by LTB4 and inhibits LTB4-induced adhesion of PMNs with an IC50 value of ~3 X 10-10 M.
|
90420 |
|
| 11-17 |
An aspirin-triggered lipoxin
5(S),6(R),15(R)-Lipoxin A4 (5(S),6(R)15(R)-LXA4) is derived from the aspirin-triggered formation of 15(R)-HETE from arachidonic acid. 5(S),6(R),15(R)-LXA4 inhibits LTB4-induced chemotaxis, adherence, and transmigration of neutrophils with twice the potency of LXA4 demonstrating activity in the nM range. The anti-inflammatory effects of aspirin may be ascribed in part to the ability of 5(S),6(R),15(R)-LXA4 to regulate leukocyte function.
|
90415 |
|
| 11-17 |
A PPARγ agonist
CAY10506 is a hybrid lipoic acid-TZD derivative that transactivates human PPARγ with an EC50 value of 10 µM.
|
10009079 |
|
| 11-17 |
Enzyme immunometric assay for the measurement of human leptin
Limit of detection:
0.5 ng/ml
·
This Enzyme Immunometric Assay (EIA) is based on a double-antibody sandwich technique. The wells of the plate supplied with the kit are coated with a polyclonal antibody specific of human leptin. This antibody will bind any Leptin introduced in the wells (sample or standard).
|
500010 |
|
| 11-17 |
An EPA-derived bronchoconstrictor
Lipoxin A5 (LXA5) is produced by enzymatic transformation of EPA by leukocytes. LXA5 slowly contracts pulmonary parenchymal strips from guinea pig with similar potency to that of LXA4 and LXB4. However, LXA5 does not exert the vasodilatory effects on aortic smooth muscle exhibited by LXA4 and LXB4.
|
10011453 |
|
| 11-15 |
A metabolite of 14,15-LTC4 with pro-inflammatory activity
14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-LOs on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. These metabolites are classified as eoxins because they are formed mostly by eosinophils. Mast cells and nasal polyps can synthesize 14,15-LTC4 as well, however metabolism to 14,15-LTE4 in these cells and tissue has not been documented. 14,15-LTE4 increases vascular permeability of human endothelial cell monolayers with about 10-fold less potency than LTC4, but approximately 100-fold greater potency than histamine.
|
10011362 |
|
| 11-15 |
A CYP450 inhibitor
4,5-diphenyl-1,2,3-Thiadiazole is, at 100 μM, an inhibitor of some CYP450 enzymes (CYP2B4, CYP1A2), but not others (CYP2E1), with inhibition occurring in a mechanism-based manner.
|
10011040 |
|
| 11-14 |
Antagonist of spingosine 1-phosphate type 1 receptor
W123 is an analog of FTY720 that is a competitive antagonist of S1P1, as measured by GTPγS activation, mitogen-activated protein kinase recruitment, cell migration, and ligand-induced receptor internalization. It has a Ki value of 0.69 μM when assessed by SEW2871-induced activation of S1P1. Its specificity for other S1P receptor subtypes remains to be determined.
|
10010992 |
|
| 11-12 |
Designed for the convenient, precise quantification of 13,14-dihydro-15-keto Prostaglandin E2
13,14-dihydro-15-keto PGE2 is the primary metabolite of PGE2 in plasma. Endogenous or infused PGE2 is rapidly metabolized by the enzymes 15-hydroxy PGDH and 15-oxo-prostaglandin Δ13-reductase to form 13,14-dh-15-keto PGE2. 13,14-dh-15-keto PGE2 accumulates to detectable levels; plasma levels in humans are between 10-100 pg/ml. It undergoes further metabolism and chemical decomposition, giving it a relatively short half-life. In dogs, the plasma half-life of 13,14-dh-15-keto PGE2 is about 9 minutes. In humans the metabolite has a similar short half-life, making it a poor choice of analytes for assays designed to measure total PGE2 biosynthesis.
|
10007214 |
|
| 11-12 |
A potent 5-HT2 receptor agonist
AL 34662 is a potent 5-HT2 receptor agonist with ocular hypotensive activity. It binds to the human and rat 5-HT2 receptors in cerebral cortex homogenates with IC50 values of 1.5 and 0.77 nM, respectively. AL 34662 binds to the recombinant human 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 14.5, 8.1, and 3 nM, respectively. In ocular hypertensive cynomolgus monkey eyes, AL 34662 lowered intraocular pressure (IOP) 25% at a dose of 100 µg and 33% at 300 µg (six hours post dose) with minimal side effects.
|
10011546 |
|
| 11-12 |
For analysis of leukotriene B4 in plasma, culture media, and other sample matrices
Sensitivity:
IC50 (50% B/B0) = 140 pg/ml; Detection Limit (80% B/B0) = 25 pg/ml
·
Cayman’s Luminex® LTB4 Kit can be used for quantification of LTB4 in plasma, culture media, and other sample matrices. This kit typically displays an IC50 (50% B/B0) of approximately 140 pg/ml and a detection limit (80% B/B0) of approximately 25 pg/ml.
|
500260 |
|
| 11-11 |
A hydrogen sulfide-releasing NSAID
ATB-337 is a hybrid molecule of an H2S donor and the NSAID diclofenac. In rats, diclofenac at 10-50 µmol/kg caused significant gastrointestinal damage, whereas no damage was observed with ATB-337 treatment at the same dose. ATB-337 at 50 µmol/kg does not promote leukocyte adherence to vascular endothelium, an effect observed with diclofenac treatment alone. COX-1 and COX-2 were inhibited with similar efficacy by diclofenac and ABT-337. An increase in expression of the pro-inflammatory mediator TNF-α, as well as, the adhesion molecules ICAM-1 and LFA-1 were not observed in rats treated with 50 µmol/kg ABT-337, effects seen with equimolar doses of diclofenac. These results indicate that H2S-releasing derivatives of NSAIDs may prove to be more effective anti-inflammatory agents than traditional NSAIDs alone.
|
10277 |
|
| 11-11 |
A precusor of sialic acid
N-Acetyl-D-mannosamine (ManNAc) is the precursor of all physiological sialic acids. Intraperitoneal injection of ManNAc twice daily at 1,000 mg/kg in C57BL/6 mice for 13 days leads to increased sialylation in kidney, liver, blood cells, brain, spinal cord, muscle, heart, lung, and spleen. ManNAc reverses hyposialylation and improves glomerular integrity in GneM712T/M712T mice whose key enzyme for sialic acid production has been deleted and may prove therapeutic in the treatment of HIBM.
|
10011060 |
|
| 11-11 |
A reversible inhibitor of H2S synthesis
β-cyano-L-Alanine (BCA) is a reversible inhibitor of the H2S synthesizing enzyme cystathionine γ lyase (CSE). BCA blocks H2S synthesis activity in rat liver preparations with an IC50 value of 6.5 µM and increases blood pressure in anaesthetized rats induced with hemorrhagic shock by inhibiting endogenous H2S synthesis. BCA at 50 mg/kg blocked both L-cysteine- and LPS-induced hyperalgesia in rats.
|
10010947 |
|
| 11-09 |
A H2S-releasing NSAID
ATB-343 is a hybrid molecule of an H2S donor and the NSAID indomethacin. In rats, ATB-343 does not cause gastric damage or promote leukocyte adherence to vascular endothelium, effects which are observed with indomethacin treatment alone. These results indicate that H2S-releasing derivatives of NSAIDs may prove to be more effective anti-inflammatory agents than traditional NSAIDs alone.
|
13045 |
|
| 11-06 |
A novel inhibitor of HIF1α protein accumulation and transcription
CAY10585 is a novel small molecule inhibitor of HIF-1α accumulation and gene transcriptional activity. In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.
|
10012682 |
|
| 11-06 |
A selective LPA1 and LPA3 receptor antagonist
Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3. It exhibits Ki values of 0.34, 6.5, and 0.93 µM for the human LPA1, LPA2, and LPA3 receptors, respectively, as determined by measuring inositol phosphate production in RH7777-transfected cells. Ki1642, at 10 µM, significantly blocks the response of a variety of cancer cell lines to LPA-induced cell migration.
|
10012659 |
|
| 11-06 |
Selective IP receptor agonist
MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM. In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs. Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor. As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.
|
10010412 |
|
| 11-05 |
Designed for the convenient, precise quantification of Bicyclo Prostaglandin E2
Bicyclo prostaglandin E2 (bicyclo PGE2) is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify it as bicyclo PGE2 to estimate PGE2 biosynthesis or metabolism in vivo.
|
10007213 |
|
| 11-05 |
Source:
human recombinant N-terminal hexahistidine-tagged protein expressed in SF21 cells
·
Mr:
67.5 kDa
·
|
10010183 |
|
| 11-05 |
Designed for the convenient, precise quantification of Prostaglandin Ethanolamide E2
Prostaglandin E2 ethanolamide (PGE2-EA) is an analog of PGE2 with improved water solubility and stability. PGE2-EA acts as an agonist with all four known EP receptor subtypes, but with an affinity that is significantly reduced compared to PGE2. PGE2 ethanolamide is produced by HCA-7 cells treated with arachidonoyl ethanolamide (AEA). The physiologic relevance of PGE2 ethanolamide is not yet established.
|
10007212 |
|
| 11-05 |
Designed for the convenient, precise quantification of Prostaglandin E2
PGE2 is one of the primary COX products of arachidonic acid and one of the most widely investigated prostaglandins. Its activity influences inflammation, fertility and parturition, gastric mucosal integrity, and immune modulation. The effects of PGE2 are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4. Affinity constants (Kd) of PGE2 for these receptors range from 1-10 nM depending on the receptor subtype and tissue.
|
10007211 |
|
| 11-03 |
A potent vasodilator
14,15-EE-(8Z)-E is a structural analog of 14(15)-EET that demonstrates potent vasodilator agonist activity in bovine coronary arteries similar to that of 14(15)-EET.
|
10010486 |
|
| 11-03 |
Designed for the convenient, precise quantification of 6-keto Prostaglandin E1
6-keto Prostaglandin E1 (6-keto PGE1) is a stable non-enzymatic hydrolysis product of prostacyclin (PGI2). 6-keto PGE1 is a metabolite isolated after the incubation of PGI2 with rabbit liver microsomes. However, it is not produced in appreciable amounts following IV infusion of PGI2 in humans. 6-keto PGE1 is equipotent with PGI2 as a vasodilator; in most other aspects its activity resembles PGE1.
|
10007210 |
|
| 10-29 |
Designed for the convenient, precise quantification of 13,14-dihydro-15-keto Prostaglandin D2
13,14-dihydro-15-keto Prostaglandin D2 (13,14-dihydro-15-keto PGD2) is a metabolite of PGD2 which is formed through the 15-hydroxy PGDH pathway. 13,14-dihydro-15-keto PGD2 was recently identified as a selective agonist for the CRTH2/DP2 receptor. It also inhibits ion flux in a canine colonic mucosa preparation. In humans, 13,14-dihydro-15-keto PGD2 is further metabolized to give 11β-hydroxy compounds which have also undergone β-oxidation of one or both side chains. Virtually no 13,14-dihydro-15-keto PGD2 survives intact in the urine.
|
10007208 |
|
| 10-29 |
A viability assay for flow cytometry
Cayman’s 7-AAD Cell Viability Assay Kit employs 7-AAD as a fluorescent label for dead cells. A fixative/actinomycin D solution is included in the kit for cell fixation and blocking, making subsequent immunostaining of surface/intracellular antigens possible. This kit provides a convenient tool to quantify cytotoxic effects of environmental toxins or drug candidates.
|
10009856 |
|
| 10-29 |
An immune modulator that is a selective S1P1 receptor agonist
KRP 203 is a selective S1P1 agonist that has been shown to reduce peripheral lymphocyte infiltration and to prolong survival in rat transplant models. The phosphorylated form of KRP 203 demonstrates a high affinity for the S1P1 with an ED50 value in the nM range and an ED50 value >1 µM for S1P3. While the immune modulating effects of KRP 203 are comparable to FTY720 (a non-selective S1P agonist), the incidence of bradycardia is reduced 10-fold with KRP 203 compared to FTY720.
|
10010426 |
|
| 10-29 |
A homolog of arachidonyl glycine
Linoleoyl glycine (LinGly) is an endogenous homolog of linoleoyl ethanolamide and arachidonyl glycine. It inhibits the hydrolysis of AEA in fatty acid amide hydrolase-containing N18TG2 cell membranes with an IC50 value of ~25 µM, which is less potent than that of arachidonyl glycine (IC50 = 7 µM). The biological significance of LinGly has not yet been determined.
|
9000326 |
|
| 10-29 |
For immunochemical detection of PCSK9
Antigen:
purified human recombinant PCSK9
·
Clone designation:
15A6
·
Host:
mouse
·
Isotype:
IgG1
·
Application(s):
PCSK9 ligand blotting (nondenaturing conditions) and WB
·
|
10218 |
|
| 10-29 |
Designed for the convenient, precise quantification of Prostaglandin D2 Ethanolamide
|
10007203 |
|
| 10-29 |
A selective inhibitor of GSK-3
SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of
31 nM. As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway.
|
10010247 |
|
| 10-27 |
96-Well assay for measurement of p53
Cayman’s p53 Transcription Factor Assay is a non-radioactive, sensitive method for detecting specific transcription factor DNA binding activity in nuclear extracts. A specific double stranded DNA (dsDNA) sequence containing the p53 response element is immobilized onto the wells of a 96-well plate. p53 contained in a nuclear extract, binds specifically to the p53 response element and is detected by addition of a specific primary antibody directed against p53. A secondary antibody conjugated to HRP is added to provide a sensitive colorimetric readout at 450 nm.
|
600020 |
|
| 10-27 |
Designed for the convenient, precise quantification of Prostaglandin D2
Prostaglandin D2 (PGD2) is a biologically active primary PG and a common product of arachidonic metabolism in mammals. PGD2 is the major eicosanoid product of mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. Mastocytosis patients produce excessive amounts of PGD2, which causes vasodilation, flushing, hypotension, and syncopal episodes. PGD2 is also produced in the brain via an alternative pathway involving a soluble, secreted PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 inhibits human ovarian tumor cell proliferation with an IC50 value of 6.8 µM.
|
10007202 |
|
| 10-24 |
Designed for the convenient, precise quantification of Prostaglandin B2
|
10007201 |
|
| 10-23 |
An inhibitor of 15-LO
15-LO inhibitor 1 is a heterocyclic pyrimidobenzothiazine compound that inhibits 15-LO with an IC50 value of 18 µM. The inhibitor appears to act as an antioxidant, interfering with the redox cycle of 15-LO.
|
10010468 |
|
| 10-23 |
Fluorescent CNGA3 channel activator
Through activation by the binding of cyclic nucleotides, cyclic nucleotide-gated (CNG) ion channels mediate sensory signal transduction in photoreceptors and olfactory cells. 8-DY547-cGMP is a fluorescently-labeled cyclic nucleotide that can be used to study CNGA2 channel activation. 8-DY547-cGMP and cGMP open the channel with equal efficiency and control of the channel activity is rapid and reversible. The difference in fluorescence (ΔF) can be determined by using DY647.
|
10010109 |
|
| 10-23 |
A long-term saturated fatty acid
Arachidic acid is a saturated fatty acid found naturally in fish and vegetable oils (such as those from peanuts). It can also be formed by the hydrogenation of arachidonic acid. Diets rich in saturated fatty acids, such as arachidic acid, are known to increase serum low-density lipoproteins resulting in high blood cholesterol levels. Because of its surfactant-like properties, arachidic acid is used in the manufacture of pharmaceuticals, soaps, cosmetics, and food packaging.
|
9000339 |
|
| 10-22 |
A derivative of phytanic acid
Phytanoyl-CoA is the conjugate of phytanic acid and coenzyme A (CoA).
|
10011499 |
|
| 10-21 |
A simple, sensitive tool for assaying aconitase from tissue homogenates and cell lysates
Cayman’s Aconitase Assay Kit provides a simple, reproducible, and sensitive tool for assaying aconitase from tissue homogenates or cell lysates. In this assay, citrate is isomerized by aconitase into isocitrate, which is then converted to α-ketoglutarate in a reaction catalyzed by isocitric dehydrogenase. These reactions are monitored by measuring the increase in absorbance at 340 nm associated with the formation of NADPH. The rate of NADPH production is proportional to aconitase activity.
|
705502 |
|
| 10-20 |
A long-chain saturated fatty acid
Docosanoic acid is a long-chain saturated fatty acid that exists naturally as a triglyceride in canola, peanut, and marine animal oils as well as animal milk fats and peanut skins. Commercially, docosanoic acid is regularly used to give hair conditioners and moisturizers their smoothing properties. As a dietary oil, docosanoic acid has poor bioavailability in humans, yet compared with oleic acid, docosanoic acid significantly raises serum total and low-density lipoproteins cholesterol concentrations.
|
9000338 |
|
| 10-17 |
An endogenous lipid with bone anabolic activity
N-Oleoyl-L-serine is an endogenous lipid that has been reported to stimulate bone formation and to inhibit bone resorption.
|
13058 |
|
| 10-16 |
A convenient fluorescence-based method for screening LSD1-specific inhibitors
Cayman’s LSD1 Inhibitor Screening Assay Kit provides a convenient fluorescence-based method for screening LSD1-specific inhibitors. The assay is based on the multistep enzymatic reaction in which LSD1 first produces H2O2 during the demethylation of lysine 4 on a peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3. In the presence of horseradish peroxidase, H2O2 reacts with ADHP to produce the highly fluorescent compound resorufin that can be analyzed with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
|
700120 |
|
| 10-15 |
Antigen:
human ApoAI amino acids 188-199
·
Clone designation:
CC3821C4
·
Host:
Mouse
·
Application(s):
WB
·
|
13042 |
|
| 10-15 |
A stable LTC4 mimetic
N-methyl Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4. Although the addition of the methyl group blocks metabolism, the biological properties of N-methyl LTC4 are somewhat reduced compared to that of LTC4. N-methyl LTC4 has a 30-fold reduced binding to LTC4 receptor-expressing DMSO-differentiated U937 cell membranes compared to LTC4 (Ki = 1,486 versus 50 nM, respectively).
|
13390 |
|
| 10-10 |
An inhibitor of platelet aggregation
Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(R)-Iloprost inhibits platelet aggregation with an IC50 value of 65 nM.
|
13076 |
|
| 10-10 |
A potent inhibitor of platelet aggregation
Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(S)-Iloprost potently inhibits platelet aggregation with an IC50 value of 3.5 nM.
|
13077 |
|
| 10-10 |
A precursor of capsaicin
8-methyl Nonanoic acid is an immediate precursor of capsaicin as well as a by-product of capsaicin degradation. Addition of 5 mM of 8-methyl nonanoic acid significantly increases the yield of capsaicin in both immobilized and freely suspended cells of C. frutescens. Capsaicin has reported antimicrobial properties, however isocapric acid can act as a growth substrate in certain bacterial strains.
|
9000310 |
|
| 10-10 |
A synthetic, pure phosphoinositol for signal transduction research
Ins(2,5,6)P3 (sodium salt) is a member of the inositol phosphate (InsP) family of second messengers that play a critical role in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3 is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. Binding of the Ins(1,4,5)P3 to its receptor on the endoplasmic reticulum results in opening of calcium channels and an increase in intracellular calcium. Ins(2,5,6)P3 is a less potent inducer of calcium release from permeabilized rat basophilic leukemia cells with an EC50 value of 110 µM compared to Ins(1,4,5)P3, which has an EC50 value of 0.17 µM.
|
10008424 |
|
| 10-10 |
A long-chain saturated fatty acid
Stearic acid is a long-chain saturated fatty acid that can be derived from either animal fats or vegetable oils. Compared to other long-chain saturated fatty acids that are hypercholesterolemic, experimental diets high in stearic acid (9.3-11.8% of energy) do not raise plasma total cholesterol or LDL-cholesterol concentrations but may slightly reduce HDL-cholesterol concentrations. Stearic acid can be used as a hardening agent for vegetable oils and due to its negligible effect on cholesterol metabolism may be used as an alternative to modification of fatty acids by partial hydrogenation.
|
10011298 |
|
| 10-06 |
A bacterial quorum sensing signal molecule
N-butyryl-L-Homocysteine thio-lactone is an analog of N-butyryl-L-homoserine lactone, the small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and cellular metabolism. N-butyryl-L-Homocysteine thio-lactone induces violacein expression in C. violaceum mutants usually not able to produce AHLs.
|
10011204 |
|
| 10-06 |
A bacterial quorum sensing signal molecule
N-octanoyl-L-Homoserin lactone (C8-HSL) is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism. The applications of this molecule include infection prevention and regulation of virulence in general and in cystic fibrosis.
|
10011199 |
|
| 09-30 |
A synthetic, pure phosphoinositol for signal transduction research
D-myo-Inositol-2,3,5-triphosphate (ammonium salt) (Ins(2,3,5)P3 (ammonium salt)) is a member of the inositol phosphate (InsP) family of second messengers that play a critical role in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3 is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. Binding Ins(1,4,5)P3 to its receptor on the endoplasmic reticulum results in opening of the calcium channels and an increase in intracellular calcium. Ins(2,3,5)P3 (ammonium salt) (tested as a racemic mixture) is 500-fold less potent than Ins(1,4,5)-P3 at initiating Ca2+ release when injected into Xenopus oocytes.
|
10008423 |
|
| 09-25 |
A bacterial quorum sensing signal molecule
N-heptanoyl-L-Homoserine lactone (C7-HSL) is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism. The diverse applications of this molecule include regulation of virulence, infection prevention, and septicemia in fish.
|
10011198 |
|
| 09-24 |
Source:
recombinant N-terminal GST-tagged SIRT1 amino acids 193-747 purified from E. coli
·
Mr:
89.2 kDa
·
|
10011190 |
|
| 09-24 |
A tumor growth inhibitor
tetramethyl Nordihydroguaiaretic acid (TMNDGA) is a synthetic derivative of NDGA, a non-selective lipoxygenase inhibitor. It inhibits Sp1 transcription factor binding at the HIV long terminal repeat promoter and at the α-ICP4 promoter, a gene essential for HSV replication, with IC50 values of 11 and 43.5 µM respectively TMNDGA induces growth arrest and apoptosis by suppressing Sp1-dependent Cdc2 and survivin gene expression giving rise to its antitumorigenic activity. The in vivo growth of xenografts in numerous human tumor types was suppressed upon treatment with TMNDGA. It also inhibits the growth of murine and human melanomas and human colon cancer in vivo without causing other tissue toxicity. TMNDGA is currently in Phase I & II clinical trials for treatment of high grade glioma brain tumors.
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70302 |
|
| 09-22 |
A specific marker of bone resorption
Glycosylated hydroxylysine residues present in bone type I collagen are terminal degradation products of the bone matrix that are released during bone resorption and excreted in the urine. 5-(galactosylhydroxy)-L-Lysine levels are elevated in patients with metabolic bone loss and thus may serve as a biochemical marker of bone collagen quality.
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10010255 |
|
| 09-19 |
A bacterial quorum sensing signal molecule
N-decanoyl-L-Homoserine lactone is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism. The applications of this molecule include regulation of virulence and exoproteases.
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10011201 |
|
| 09-19 |
Source:
recombinant protein purified from E. coli
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Mr:
23 kDa (α subunit) 26.5 kDa (β subunit)
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|
10011353 |
|
| 09-18 |
A potent antiproliferative rotenoid compound
The rotenoid compound deguelin, originally isolated from the bark of M. sericea (Leguminosae) to be used as an insecticide and fish poison, has chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis. Deguelin inhibits cell growth (IC50 = <10-8 M), blocks PI3K/Akt activation, suppresses COX-2 expression, and induces apoptosis in premalignant and squamous human bronchial epithelial (HBE) cells without affecting normal HBE cells. At 6 mg/kg, deguelin induces Parkinson’s disease-like symptoms in rats after six days of subcutaneous infusion, and therefore may also serve as a useful model for Parkinson’s disease research.
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10010706 |
|
| 09-18 |
A small molecule activator of p53
Tenovin-1 is a small molecule activator of p53 transcriptional activity. At 10 µM, it elevates p53 expression in MCF-7 cells within two hours of treatment and longer-term exposure significantly decreases the growth of BL2 Burkitt’s lymphoma and ARN8 melanoma cells. Functioning upstream of p53, tenovin-1 acts by inhibiting the deacetylase activity of purified human SIRT1 and SIRT2, members of NAD+-dependent class III histone deacetylases that belong to the sirtuin family. While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo.
|
13085 |
|
| 09-18 |
A cGMP phosphodiesterase inhibitor
Zaprinast, the compound from which sildenafil (Viagra™) was developed, is a cGMP-specific phosphodiesterase inhibitor. It moderately inhibits PDE5 and PDE6 with IC50 values of 0.5-0.76 and 0.15 µM, respectively, and weakly inhibits PDE9, PDE10, and PDE11 with IC50 values of 35, 22, and 11-33 µM, respectively. Zaprinast therefore enhances the vasodilatory effects of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase. Zaprinast also activates both the rat and human G protein-coupled receptor, GPR35 with EC50 values of 16 nM and 0.84 µM, respectively.
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10010421 |
|
| 09-15 |
A selective CK2 inhibitor
NSC 210902 inhibits CK2 with an IC50 value of 1 µM and competitively inhibits binding of ATP with a Ki value of 0.28 µM. NSC 210902 is selective for CK2 as it only minimally inhibits the activities of other protein kinases (e.g., JNK3, GSK3, CDK5, and MSK1).
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10011255 |
|
| 09-15 |
Antigen:
human PDCD4 C-terminal amino acids 458-468 (GDGGRLKPESY)
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Host:
rabbit
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Application(s):
WB
·
|
10250 |
|
| 09-08 |
A potent and selective inhibitor of IKK-ε
The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKKα and IKK-β, can also activate NF-κB. IKK-ε is expressed predominantly in immune cells, and is thought to play a role in the immune response. CAY10576 is a benzimidazole analog that selectively inhibits IKK-ε with an IC50 value of 40 nM and is essentially inactive at IKK-α and IKK-β.
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10011249 |
|
| 09-05 |
A convenient fluorescence-based method for screening FAAH inhibitors
Cayman’s FAAH Inhibitor Screening Assay Kit provides a convenient fluorescence-based method for screening FAAH inhibitors. FAAH hydrolyzes AMC-arachidonoyl amide resulting in the release of the fluorescent product, 7-amino-4-methylcoumarin (AMC). The fluorophore can be easily analyzed using an excitation wavelength of 340-360 nm and an emission wavelength of 450-465 nm.
|
10005196 |
|
| 09-05 |
Cayman’s Glycerol Cell-Based Assay Kit provides a convenient tool for studying triglyceride/fatty acid cycling and its regulation in adipocytes or hepatocytes. This kit will allow users to screen compounds in |
