12 products were found matching "Cay15145"!

Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport. It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by...

Chymostatin is a bioactive peptide of microbial origin that acts as a protease inhibitor with selectivity for chymotryptase-like serine proteases. It potently inhibits chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively) while less effectively blocking the activity of cathepsins, papain, and leukocyte...

Nelfinavir is an orally bioavailable inhibitor of the HIV-1 protease (Ki =2 nM). It demonstrates anti-cancer activity, selectively preventing the growth of HER2-positive breast cancer cells in vitro by inhibiting Hsp90 (IC50 = 3.1 µM). Formulations containing nelfinavir have been used in combination with HIV reverse...

LY303511 is a close structural analog of LY294002 (Cay-70920), a selective phosphatidylinositol 3-kinase (PI3K) inhibitor. LY303511, however, does not inhibit PI3K-dependent phosphorylation of Akt but instead has been shown to inhibit mTOR-dependent phosphorylation of S6K. It can reduce cell proliferation in human...

Cyclin-dependent kinase 1 (Cdk1) complexes with different cyclins, with the cyclin determining substrate specificity. Ro 3306 is a cell-permeable, reversible inhibitor of Cdk1, showing preference for Cdk1/cyclin B1 (Ki = 35 nM) over Cdk1/cyclin A (Ki = 110 nM), two CDK complexes which regulate cell cycling. It also...

Abiraterone acetate is an inhibitor of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 17 and 18 nM for inhibition of C17,20-lyase and 17alpha-hydroxylase activities, respectively). It is also a prodrug form of abiraterone (Cay-9002768). Abiraterone acetate reduces plasma testosterone levels, increases plasma...

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer. Mutations in the kinase B-Raf are involved in a wide range of cancers. In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of...

PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease. It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 µM. PF-429242 completely inhibits proteolytic...

Corticotropin-releasing hormone (CRH) secreted from the hypothalamus is the major regulator of pituitary corticotropin-release and consequent glucocorticoid secretion. Antalarmin is a selective, nonpeptide antagonist of the CRH receptor 1 (Ki = 1 nM) that, consequently, reduces the release of corticotropin in...

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-gamma. JAK Inhibitor I is a pyridine-containing...

Roflumilast is an inhibitor of phosphodiesterase 4 (PDE4, IC50 = 0.8 nM). It is selective for PDE4 over PDE1, -2, -3, and -5 (IC50s = >10, >10, >10, and 8 µM, respectively). Roflumilast inhibits the production of leukotriene B4 (LTB4, Cay-20110) induced by fMLP (Cay-21495) in isolated human neutrophils with an IC50...

Z-Asp-CH2-DCB is a peptide originally synthesized for its ability to inactivate the interleukin-1beta-converting enzyme, which is the homolog of the C. elegans positive regulator of apoptosis CED-3. Z-Asp-CH2-DCB has been shown to block apoptosis by nonselectively inhibiting caspase activity. At 1-100 µM, it can...