12 products were found matching "Cay13250"!

KIAA1363 is a 2-acetyl monoacylglyceryl ether (MAGE) hydrolase that is upregulated in aggressive cancers from various tissues. The enzyme catalyzes the hydrolysis of the 2-acetyl MAGE to MAGE and serves as a central enzyme in the PAF and LPA signaling network. AS 115 is a potent and selective inactivator of...

2-Acetyl-5-tetrahydroxybutyl imidazole (THI) is an inhibitor of sphingosine-1-phosphate (S1P) lyase in vivo. THI is not active at S1P lyase in cell-free or cell-based assays but is converted to A6770 in vivo, which is subsequently activated by phosphorylation. In mice, THI (50 µg/ml in drinking water) increases S1P...

Two Rho-associated kinases (ROCK), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent...

Formation of cis monoenoic acids from unsaturated fatty acids, such as palmitoleic acid (9-cis-hexadecenoic acid) from palmitic acid occurs readily in animal tissues. Delta2-trans-Hexadecenoic acid is an intermediate formed in the beta-oxidation of palmitic acid. In a model meant to simulate gastric ulceration,...

Tamoxifen is an estrogen receptor antagonist (IC50 = 45 nM for the rabbit receptor). It reduces the proliferation of MCF-7 breast cancer cells when used at a concentration of 10 µM. Tamoxifen is active against S. cerevisiae, C. neoformans, and five Candida species (MICs = 12, 64, and 8-64 µg/ml, respectively). It...

DEPMPO is a nitrone that is used to spin trap reactive O-, N-, S-, and C-centered radicals and allow their characterization when used in association with electron spin resonance. It is noted for the stability of adducts formed. DEPMPO can be used in vitro or in vivo, as it crosses lipid bilayer membranes and is a...

Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM). It binds to 14-alpha sterol demethylase/CYP51 isoform B (AF51B, Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation). It inhibits...

ThioGlo1 is a thiol-reactive fluorescent probe. Upon reaction with a thiol group, a fluorescent adduct is formed that displays excitation/emission maxima of 384/513 nm, respectively. It also reacts with sulfite to form a fluorescent adduct with similar spectral characteristics, and interference from sulfite during...

Agomelatine is an agonist of melatonin (MT) receptors and a derivative of melatonin (Cay-14427). It binds to MT1 and MT2 receptors (Kis = 0.14 and 0.41 nM, respectively) and has an EC50 value of 0.1 nM in a [35S]GTPgammaS binding assay using CHO cells expressing MT2 receptors. Agomelatine is also an antagonist of...

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production,...

URB447 is a cannabinoid 1 (CB1) receptor antagonist and CB2 receptor agonist. It inhibits the binding of the CB receptor agonist [3H]-WIN 55,212-2 to CHO-K1 cells expressing the human CB2 receptor or rat cerebellar membranes (IC50s = 41 and 313 nM, respectively). URB447 (20 mg/kg) reduces food intake and weight gain...

FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion. In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM). In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that...