chmfl-bmx-078

Description: CHMFL-BMX-078 is a highly potent and selective type II irreversible/covalent kinase inhibitor of BMX (bone marrow kinase on chromosome X) kinase with an IC50 of 11 nM. CHMFL-BMX-078 exhibits an IC50 of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC50=437 nM). BMX is a member of TEC family nonreceptor tyrosine kinase and is involved in a variety of critical physiological and pathological processes. Given the fact that BMX mediated signaling pathway is still not fully understood, CHMFL-BMX-078 would serve as a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways.

References: J Med Chem. 2017 Mar 9; 60(5):1793-1816.