9 products were found matching "Cay16240"!

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...

Ezatiostat is an inhibitor of glutathione S-transferase pi 1-1 (GSTP1-1, Ki = 0.4 µM). It is selective for GSTP1-1 over GSTalpha and GSTµ family GSTs (Kis = 20-75 µM). Ezatiostat also inhibits the protein-protein interaction between GSTP1-1 and JNK1. In vivo, ezatiostat (75 mg/kg) increases the number of circulating...

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mutated kinase (ATM) and ataxia-telangiectasia and Rad3-related kinase (ATR) in a study that has since been retracted.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...

The family of Pim (Provirus Integration site for Moloney murine leukemia virus) proteins are serine/threonine kinases involved in cell survival and cell proliferation. CX-6258 is a potent, reversible inhibitor of Pim-1, -2, and -3 (IC50s = 5, 25, and 16 nM, respectively). It demonstrates excellent selectivity,...

CK-636 is an inhibitor of Arp2/3 complex action that binds the complex and inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC50s = 4, 32, and 24 µM, respectively). It is cell permeable, as it prevents actin polymerization and the formation of actin filament comet tails by...

CO-1686 is an irreversible kinase inhibitor that specifically targets mutant forms of the epidermal growth factor receptor (EGFR) including T790M (Ki = 21.5 nM) with significantly reduced activity at the wild-type form of the receptor (Ki = 303.3 nM). CO-1686 has been shown to inhibit the proliferation of non-small...

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....

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are highly specific and potent allosteric inhibitors of HIV-1 reverse transcriptase. Dapivirine, a diarylpyrimidine derivative of the potent NNRTI efavirenz (Cay-14412), inhibits HIV-1 reverse transcriptase with an IC50 value of 24 nM in vitro. It impedes the...

Foretinib is a broad-spectrum tyrosine kinase (TK) inhibitor that targets members of the HGF and VEGF receptor TK families, as well as KIT, Flt-3, PDGFRbeta, and Tie-2, at nanomolar concentrations. It blocks HGF-induced Met phosphorylation and VEGF-induced ERK phosphorylation, preventing HGF-induced responses in...