BMX-IN-1

Description: BMX-IN-1 is a novel, potent, selective and covalent / irreversible BMX (bone marrow tyrosine kinase on chromosome X) inhibitor with the potential for treating prostate cancer. BMX-IN-1 can covalently modifies Cys496. It targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity. BMX-IN-1 inhibits the proliferation of Tel-BMX-transformed Ba/F3 cells at two digit nanomolar concentrations but requires single digit micromolar concentrations to inhibit the proliferation of prostate cancer cell lines.

References: https://pubs.acs.org/doi/abs/10.1021/cb4000629