12 products were found matching "Cay160112-%25"!

Chenodeoxycholic acid (CDCA) is a hydrophobic primary bile acid. It is formed from cholesterol in the liver via a multistep process catalyzed by the cytochrome P450 (CYP) isoforms CYP7A1, CYP8B1, and CYP27A1. CDCA is a farnesoid X receptor (FXR) agonist that binds to FXRs in a TR-FRET assay (EC50 = 13 µM) and...

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,...

Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human...

Casein Kinase 2 (CK2) is a constitutive protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. CAY10578 is a potent inhibitor of CK2 with an...

Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism. They are also inherently cytotoxic, as physiological...

Bone morphogenetic proteins (BMP) are secreted signaling proteins, many of which are involved in various developmental processes, in addition to bone formation. GDF11 is a circulating growth and differentiation factor that has age-dependent effects on development. Notably, injection of recombinant GDF11 into old...

Enzastaurin is a potent inhibitor of PKCbeta (IC50 = 6 nM), with modest selectivity over PKCalpha, PKCgamma, and PKCepsilon (IC50 = 39, 83, and 110 nM, respectively). At 3 µM, enzastaurin also inhibits signaling through the Akt pathway. It suppresses angiogenesis, induces apoptosis, and reduces proliferation of...

Leukotrienes (LTs) are a group of acute inflammatory mediators derived from arachidonic acid in leukocytes. The majority of these metabolites are formed through the 5-lipoxygenase (5-LO) pathway. 14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the...

ST1535 is an adenosine A2A receptor antagonist. It is selective for adenosine A2A over A1 receptors (Kis = 2.3 and 107 nM, respectively, in radioligand binding assays). ST1535 inhibits agonist-induced production of cAMP in CHO cells expressing adenosine A2A receptors (IC50 = 353 nM). In vivo, ST1535 (10 and 20...

Phenoxybenzamine is an antagonist of alpha-adrenergic receptors (alpha-ARs). It inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing alpha1-ARs (EC50s = 125.9-316.2 nM), as well as radioligand binding to alpha2A-, alpha2B-, and alpha2C-ARs in CHO cell membranes (Kis = 60, 10, and...

8-CPT-Cyclic AMP is a lipophilic activator of the cyclic-AMP- and cyclic-GMP-dependent protein kinases, PKA and PKG (Ka = 0.05 and 0.11 µM, respectively). 8-CPT-cAMP inhibits cyclic GMP-specific phosphodiesterase (PDE VA), cyclic GMP-inhibited phosphodiesterase (PDE III), and cyclic AMP-specific phosphodiesterase...

1-Palmitoyl-2-hydroxy-sn-glycero-3-PE is a naturally occurring lysophospholipid. It inhibits the growth of L. donovani promastigotes (GIC50 = 8 µM). 1-Palmitoyl-2-hydroxy-sn-glycero-3-PE serum levels are decreased in a mouse model of alcohol-induced liver injury and in a hepatocellular carcinoma mouse xenograft...