14 products were found matching "Cay16250"!

5-trans PGF2beta is the 9beta-hydroxy isomer of 5-trans PGF2alpha. There are no published reports on the biological activity of this compound.Formal Name: 9beta,11alpha,15S-trihydroxy-prosta-5E,13E-dien-1-oic acid. CAS Number: 36150-02-4. Synonyms: 5-trans-9beta-Prostaglandin F2alpha, 5,6-trans PGF2beta. Molecular...

Pimozide is a dopamine receptor antagonist (Kis = 2.4, 0.3, and 1.8 nM for D2, D3, and D4 receptors, respectively). It also binds to eight additional receptors (Kds = 25-3,100 nM for the human receptors) and inhibits the voltage-gated sodium channel Nav1.2 and the voltage-gated potassium channel Kv11.1 (IC50s = 42...

Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII,...

AZD 9291 is an inhibitor of mutant EGFRs (IC50s = 1, 12, and 5 nM for EGFRL858R/T790M, EGFRL858R, and EGFRL861Q, respectively). It is selective for these mutant EGFRs over wild-type EGFR (IC50 = 184 nM), as well as over a panel of approximately 280 other kinases at 1 µM. AZD 9291 selectively inhibits the...

Smoothened (Smo) is a cell surface receptor that, with Patched, mediates sonic hedgehog (Shh) signaling to regulate gene expression through the Gli transcription factors. BMS 833923 is an orally bioavailable inhibitor of Smo. It blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell...

Bruton's tyrosine kinase (BTK) is a member of the BTK/Tec family of protein tyrosine kinases involved in signal transduction pathways regulating proliferation, survival, migration, and tissue homing of B-cells. Ibrutinib is an irreversible inhibitor of BTK (IC50 = 0.5 nM) that selectively blocks B cell activation,...

Dimetridazole is a nitroimidazole-based compound with antibacterial and anticoccidial activity. It was once widely used in the treatment of parasitic infections in poultry, cattle, swine and farmed fish until suspected to be carcinogenic and mutagenic to humans. Hydroxy dimetridazole is a metabolite of dimetridazole...

CGK733 is an anticancer compound that was originally identified as an inhibitor of ataxia-telangiectasia mutated kinase (ATM) and ataxia-telangiectasia and Rad3-related kinase (ATR) in a study that has since been retracted. It inhibits irradiation-induced activation of ATM in a reporter assay using HEK293 cells when...

CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively). It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM). At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines....

GNF-5 is an allosteric inhibitor of Bcr-Abl (IC50 = 0.121 µM) and a derivative of GNF-2 (Cay-16253). It also inhibits the Bcr-Abl mutants Bcr-AblG250E, Bcr-AblE255V, and Bcr-AblM351T (IC50s = 4.52, 0.38, and 0.93 µM, respectively). GNF-5 inhibits the growth of Ba/F3 cells (IC50 = 0.145 µM). It reduces viral titers...

The proto-oncogene serine/threonine-protein kinases, Pim-1 and Pim-2, are enzymes involved in cytokine signaling and participate in various signal transduction pathways, including cell growth, differentiation, and apoptosis. Their overexpression has been implicated in prostate cancer, some forms of leukemia, and...

ATB-346 is a non-steroidal anti-inflammatory drug (NSAID) that releases hydrogen sulfide (H2S) and a derivative of naproxen (Cay-70290). It inhibits the proliferation of, and induces apoptosis in, A375 melanoma cells when used at a concentration of 100 µM. ATB-346 decreases prostaglandin E2 (PGE2) production in...