[CAS NO. 1808288-51-8]  CHMFL-BMX-078

Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC ₅₀ 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 (IC ₅₀ =437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding K _d of 81 nM, while for the active state of BMX kinase, it exhibits a binding K _d of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI ₅₀ =0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC ₅₀ =5.8 nM) than C496S mutant (EC ₅₀ =459 nM) for the inhibition of BMX total tyrosine phosphorylation. CHMFL-BMX-078 would serve as a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.