8 products were found matching "Cay17501"!

Cytosporone B is a naturally occurring agonist for the nuclear receptor Nur77 (IC50 = 0.278 nM). Activation of Nur77 with cytosporone B induces the expression of Nur77-dependent genes, including the gene for Nur77 itself. Signaling through Nur77 induces apoptosis in cancer cells and retards xenograft tumor growth....

BHPI is an antagonist of estrogen receptor alpha (ERalpha) that blocks 17beta-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM. It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a...

JWH 307 (Cay-10797) is a (1-naphthoyl)pyrrole cannabimimetic that potently activates both the central cannabinoid (CB) receptor, CB1, and the peripheral CB2 receptor (Ki = 7.7 and 3.3 nM, respectively). JWH 307 3'-isomer differs from JWH 307 by having the fluorophenyl group at the 3' position, rather than the 2'...

Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins. It is much less effective or...

BMS 754807 is a reversible, orally bioavailable dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases (IC50s = 1.8 and 1.7 nM, respectively). It has minimal effect against an array of other tyrosine and serine/threonine kinases. BMS 754807 inhibits cell...

The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive...

Lipoprotein-associated phospholipase A2, also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7, hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities....

Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and CAII. It inhibits COX-2 in the absence of carbonic anhydrase II with an IC50 value of 40 nM, which increases by approximately 4- and 17-fold in the presence of a CAII at a molar ratio of 1:1 and 1:5, respectively....