11 products were found matching "Cay14865"!

alpha-Truxillic acid can be formed by the dimerization of two molecules of alpha-trans-cinnamic acid. It is related to incarvillateine, a natural antinociceptive compound derived from the Asian herb I. sinensis. alpha-Truxillic acid and some of its derivatives significantly block inflammatory pain while having...

Silodosin is a potent alpha1A-adrenoceptor antagonist (Ki = 0.036 nM). It shows selectivity for the prostatic adrenoceptor. As a result, it is effective against lower urinary tract symptoms associated with benign prostatic hyperplasia.Formal Name:...

Amlodipine is a dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle. Acting as a vasodilator, amlodipine reduces blood pressure by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance. It inhibits...

Akt functions as a key component in multiple signaling pathways to promote cell survival by mediating resistance to apoptosis. Akt inhibitor X is a cell permeable phenoxazine derivative that suppresses insulin-like growth factor 1 (IGF-1)-stimulated phosphorylation of Akt with an IC50 value of 1-2 µM. This compound...

Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM, IC50 = 0.09 nM for the human receptor). It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3). In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P...

PS-1145 is an IkappaB kinase beta (IKKbeta) inhibitor (IC50 = 88 nM). It selectively inhibits IKKbeta over a panel of 14 kinases (IC50s = >100 nM for all). PS-1145 also inhibits the IKK complex (IC50 = 100 nM). It inhibits the proliferation of MM.1S, U266, and RPMI-8226 myeloma cells when used at concentrations...

Marimastat is a broad-spectrum matrix metalloproteinase (MMP) inhibitor (IC50s = 5, 6, 230, 16, and 3 nM for MMP-1, MMP-2, MMP-3, MMP-7, and MMP-9, respectively). It also binds to a recombinantly expressed catalytic domain of human MMP-14 (MMP-14cat, Ki = 2.1 nM) and inhibits gelatinases (IC50s = 3-6 nM), fibroblast...

MET is a proto-oncogene which encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. SU11274 is a potent, selective, ATP-competitive inhibitor of c-Met (IC50 = 20 nM). It has much less...

Leflunomide is a synthetic isoxazol and a prodrug form of A-771726 (Cay-14404), a dihydroorotate dehydrogenase inhibitor. Leflunomide inhibits de novo pyrimidine synthesis to regulate T lymphocyte progression through the cell cycle. It inhibits proliferation and activation of T cells when used at concentrations of...

Vatalanib is an antagonist of the VEGF receptors, inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC50 values of 77, 37, and 190 nM, respectively. It less potently inhibits PDGF and c-Kit (IC50 = 600 and 700 nM) and has no effect on a large panel of...

Ciprofloxacin is a fluoroquinolone antibiotic. It is active against a variety of Gram-positive and Gram-negative bacteria in vitro, including S. aureus, L. monocytogenes, P. aeruginosa, Legionella, N. gonorrhoeae, and H. pylori (MIC50s = 0.004-1 µg/ml). It is also active against clinical isolates of Bacteroides,...