9 products were found matching "Cay16615"!

BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP, IC50s = 0.09-1.7 µM). It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide. Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values...

JWH 122 is a synthetic cannabinoid (CB) that displays high affinities for both the central CB1 receptor (Ki = 0.69 nM) and the peripheral CB2 receptor (Ki = 1.2 nM). JWH 122 N-(4-pentenyl) analog is structurally related to JWH 122, differing only by the presence of a terminal double bond on the acyl chain. This...

N-Acetyl-4-benzoquinone imine (NAPQI) is a cytochrome P450 3A4 and 2E1 metabolite of acetaminophen that can be toxic to the liver when acetaminophen is consumed in large doses. At therapeutic doses of acetaminophen, NAPQI is inactivated by conjugation with glutathione. However, following toxic doses of...

Angiotensin II is a peptide hormone which regulates blood pressure and fluid balance, contributing to hypertension, atherosclerosis, left ventricular hypertrophy, myocardial infarction, and heart failure. Telmisartan is a nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the...

Estradiol 3-(beta-D-glucuronide) (E23G) is a non-cholestatic regioisomer of the estrogen metabolite, estradiol 17-(beta-D-glucuronide) (E217G, Cay-16156). It acts as a substrate for multidrug resistance protein 2 (MRP2, Km = 122 µM), competing with E217G for MRP2-mediated transport (IC50 = 14.2 µM). E23G has been...

UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively). It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases. UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines...

SET domain-containing protein 8 (SETD8) is a methyltransferase that selectively monomethylates histone H4 at lysine residue 20 (H4K20), an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor....

TGF-beta is a cell growth and differentiation factor that has roles in cancer, fibrosis, and numerous other pathologies. TGF-beta signals through two receptor tyrosine kinases, TGF-betaRI and TGF-betaRII. SD 208 is a potent inhibitor of TGF-betaRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of...

3'-Sialyllactose consists of the monosaccharide N-acetylneuraminic acid linked to the galactosyl subunit of lactose at the 3 position. It is an abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum. 3'-Sialyllactose avidly binds several viral strains, including...