15 products were found matching "Cay10009597"!

Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively). It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM. Flavopiridol inhibits transcription of a CMV promoter in HeLa...

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1,...

The NMDA receptor (NMDAR) plays an essential role in memory, neuronal development, and it has also been implicated in several disorders of the central nervous system including Alzheimer's disease, epilepsy, and ischemic neuronal death. The NR1 protein can form NMDA activated channels when expressed in Xenopus...

Formulation: 1 ml of propidium iodide reagent.

The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor. CAY10509 is an analog of PGF2alpha containing a thio-fluorobenzene substituent in the lower side chain. CAY10509 has an IC50 of about 30 nM...

Calcipotriol (hydrate) is a low-calcemic vitamin D receptor (VDR) agonist. Calcipotriol (hydrate) is about 200 times less potent in its effects on calcium metabolism than vitamin D (1,25[OH]D3). Binding of calcipotriol (hydrate) to the VDR increases AP-1, a transcription factor important for keratinocyte...

Pseudomonas aeruginosa (P. aeruginosa) is a common pathogen affecting immunocompromised patients with acute diseases such as pneumonia and vasculitis or chronic diseases such as cystic fibrosis. It produces several phenazine toxic metabolites, the most predominant of which is a blue pigment, pyocyanin. Pyocyanin,...

6,7-dihydroxy Bergamottin (6,7-DHB) is a potent inhibitor of CYP3A4 (IC50 = 25 µM). It appears to be the primary compound in grapefruit juice that is responsible for inhibition of testosterone 6beta-hydrolase activity. Ingestion of grapefruit juice during treatment regimes with drugs normally metabolized by...

Taranabant is a cannabinoid (CB) receptor 1 inverse agonist (Ki = 0.13 nM). It is selective for CB1 over CB2 receptors (Ki = 170 nM), as well as a panel of 170 receptors, enzymes, ion channels, and transporters at 1 µM. Taranabant increases forskolin-induced cAMP production in CHO cell membranes expressing human CB1...

Formulation: 25 or 125 mg of MTT powder.

Prorenin is the inactive precursor of renin, which is a key enzyme in the regulation of blood pressure and electrolyte balance. In renal juxtaglomerular cells, sequential cleavage of the N-terminal 20 and 46 amino acids of preprorenin produces prorenin and active renin, respectively. Renin catalyzes the conversion...

Arachidonoyl ethanolamide (AEA, anandamide) is an endogenous lipid neurotransmitter with cannabinergic activity, binding to both the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. Fatty acid amide hydrolase (FAAH) is the enzyme responsible for the hydrolysis and inactivation of AEA. Metabolism...