tcsc1295 BMX-IN-1

BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys⁴⁹⁶ in the BMX ATP binding domain with 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.

IC50 & Target: IC50: 8 nM (BMX), 10.4 nM (BTK)

In Vitro: BMX-IN-1 inhibits the proliferation of Tel-BMX-transformed Ba/F3 cells and RV-1 cells with IC₅₀s of 25 nM and 2.53 μM. BMX-IN-1 exhibits remarkable selectivity with an S(10) score of 0.01. BMX-IN-1 inhibits only wild-type BMX with an IC₅₀ of 138 nM. BMX-IN-1 requires covalent modification of Cys⁴⁹⁶ of BMX to achieve potent inhibition^[1].