Cayman Chemical

A major metabolite produced from testosterone by the actions of CYP3A4 and CYP3A5.

The orally active metabolite of the non-sedating antihistamine loratadine; an antagonist of the histamine H1 receptor (Ki = 0.97 nM).

CCT251545 is an orally bioavailable inhibitor of Wnt signaling (IC₅₀ = 5 nM). It is a potent and selective inhibitor of the human mediator complex-associated protein kinases Cdk8 and Cdk19. Through its effects on Cdk8 and Cdk19, CCT251545 alters Wnt pathway-regulated gene expression. It...

A competitive antagonist of S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively); inhibits S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.

Source: Recombinant protein expressed in E. coli Mr: 15.5 kDa Histone H3 is one of the core nucleosomal histones. It undergoes many modifications which include acetylation, methylation, and phosphorylation that are important for regulation of gene transcription.

A quinolone antibiotic that inhibits the integrase of HIV-1 (IC₅₀ = 7.2 nM); blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer.

A selective inhibitor of STAT3 activation, dimerization and nuclear translocation (IC₅₀ = 5.1 μM at 37°C); 10 μM induces apoptosis in STAT3-dependent breast cancer cells.

A very long chain fatty acid (24:1n-9) enriched in nervous tissue and particularly abundant in sphingolipids, such as sphingomyelin; poorly produced in demyelinating disorders, including multiple sclerosis and adrenoleukodystrophy; binds and inhibits DNA polymerase β (Ki = 4.0 uM) and HIV-1...

A pyrazine derivative that is used as a flavoring agent in the food and tobacco industry; has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC₅₀ = ~1.25 mM).

An intermediate aldehyde metabolite of losartan that does not block angiotensin receptors, but instead inhibits COX-2 expression, blocks ICAM-1 mRNA upregulation, and COX-dependent generation of TXA2 and PGF2α; also acts as a partial agonist (EC₅₀ = 17.1 µM) of PPARγ.

A potent, selective PPARα agonist that activates murine and human PPARα with EC50 values of 0.005 and 0.05 µM, respectively; 0.2 mg/kg given orally once daily for three days decreased serum total LDL cholesterol 40-60% in male Sprague-Dawely rats.

An inhibitor of p53-mediated apoptosis, preventing p53 binding at the mitochondrial surface without affecting p53 transactivational activities; at 25 μM, pifithrin-μ reduces p53-mediated apoptosis triggered by nutlin; also interacts selectively with HSP70, disrupting its association with many...

A fatty acyl amide of taurine discovered during MS lipidomic analysis of rat brain.

An analog of adenosine used to prepare nucleoside derivatives as inhibitors of viral RNA translation and replication.

Lyso-PAF C-18 can be formed by either the action of PAF-AH on PAF C-18 or by the action of a CoA-independent transacylase on 1-O-octadecyl-2-acyl-glycerophosphocholine. Lyso PAF C-18 is a substrate for eitherPAF C-18 formation by the remodeling pathway or selective acylation with arachidonic acid by...

A selective, orally available inhibitor of MEK1 (IC₅₀ = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.

An orally bioavailable inhibitor of ALK (IC₅₀ < 100 nM in Ba/F3 cells); a pan-ALK inhibitor that also inhibits several ALK mutants that confer resistance to other ALK inhibitors.

A celecoxib analog that retains potent, selective COX-2 inhibitory activity (IC50 = 32 nM).

A potent, selective DP2 antagonist (Kis = 13, 3, and 4 nM for human recombinant DP2, rat recombinant DP2 receptors, and human native DP2 from Th2 cell membranes, respectivley); inhibits chemotaxis and cytokine production of human Th2 lymphocytes with IC50 values of 28 and 19 nM, respectively;...

A dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC₅₀ = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and...

8-iso Misoprostol is one of several possible impurities in the production of bulk commercial preparations of misoprostol, and one that is somewhat difficult to distinguish from other impurities such as 11β-misoprostol. The pharmacology and EP receptor binding affinity for 8-iso misoprostol has...

A heptadecapeptide that acts as an endogenous opioid receptor agonist (Kis = 0.5-1 nM for κ, µ, and δ); has been implicated in antinociceptive functions.

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of...

A cell-permeable inhibitor of HIF-1-mediated gene transcription which acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the HRE; reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50 value...