16 products were found matching "Cay14710"!

15(R)-Prostaglandin E2 (15(R)-PGE2) is the C-15 epimer of the naturally occurring 15(S)-PGE2. 15(R)-PGE2 is much less potent than the natural stereoisomer in most biological assays. In hamsters, a dose of 0.20 mg of PGE2 (Cay-14010) inhibits fertility by 100%, whereas a dose of 1.0 mg of 15(R)-PGE2 inhibits...

3'-fluoro-alpha-PPP is a derivative of alpha-PPP, characterized by the addition of a fluorine group at the 3 position of the phenyl ring. The physiological and toxicological properties of this compound are not known. This product is intended for forensic and research applications.Formal Name:...

Recognition of epigenetic marks can be mediated by small modular protein units of ~50 amino acids called Plant Homeodomain (PHD) fingers. PHD fingers are zinc binding domains that have a Cys4-His-Cys3 motif and are found in more than 100 nuclear proteins that play a role in regulating chromatin. PHD domains often...

Posaconazole is a broad-spectrum triazole antifungal agent active against various yeasts and molds, including Aspergillus, Candida, Fusarium, and Zygomycetes. Posaconazole inhibits the growth of fungi by inhibiting the lanosterol 14alpha-demethylase enzyme (IC50s = 7-200 nM), which results in a disruption in the...

2C-E, known formally as 2,5-dimethoxy-4-ethyl phenethylamine, is a psychoactive compound that is regulated as Schedule I in the United States. 25E-NBOMe is a derivative of 2C-E having an N-(2-methoxybenzyl) addition at the amine. This addition on related phenethylamines increases the affinity and selectivity for the...

25I-NBOMe, a derivative of the serotonin 2A (5-HT2A) receptor agonist 2C-I, is 16-fold more potent than 2C-I with a Ki value of 0.044 nM for human 5-HT2A receptors. 25I-NBOMe 3-methoxy isomer differs from 25I-NBOMe by having a methoxy group at the three, rather than two, position on the benzene ring. The properties...

Vildagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4, Ki = 0.003 µM). It is selective for DPP-4 over DPP-2, DPP-8, and DPP-9 (Kis = >500, 0.81, and 0.095 µM, respectively). Vildagliptin (3 mg/kg) decreases plasma glucose levels and increases plasma insulin levels during an oral glucose challenge in Zucker...

Vandetanib is a multi-kinase inhibitor that inhibits VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRbeta, Tie-2, and FGFR1 in cell-free assays (IC50s = 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively). It also binds to 142 additional kinases in a panel of 442 kinases (Kds = 4.6-7,900 nM). Vandetanib (1 and 2.5 µM)...

FSLLRY-amide is a peptide antagonist of protease-activated receptor (PAR) 2 which blocks activation by trypsin (IC50 = ~50 µM) but not by the synthetic agonist SLIGRL-NH2 (Cay-16723). It does not affect thrombin-induced activation of PAR1 or trypsin-mediated proteolysis of casein. It can be used to study PAR2 action...

3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM). It less effectively inhibits a panel of...

The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers. PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM, IC50 = 9 nM). It exhibits >50-fold selectivity...

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM. It also induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells. WP1066 is...