A selective inhibitor of phosphoinositide 3-kinase α (PI3Kα)
BYL719 is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM). It is less effective against PI3K isoforms β, γ, and δ as well as a range of related kinases. BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice. Learn more.
A library of epigenetic probes from the Structural Genomics Consortium (SGC)
The SGC, in conjunction with academic and industrial partners, has developed numerous small, drug-like molecules that inhibit or antagonize epigenetic readers, writers, and erasers. We provide these probes as part of our expanding epigenetics product portfolio. The SGC Probe Set contains a collection of these compounds each packaged as a 1 mg sample size for ease of preclinical target validation during early stages of drug discovery. Learn More.
A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme. It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils. Learn More.
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Small Molecule Inhibitors Selection Guide
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