BMX-IN-1 is a selective, irreversible inhibitor ofbone marrow tyrosine kinase on chromosome X (BMX)that targets Cys⁴⁹⁶in the BMX ATP binding domain with anIC₅₀of 8 nM, also targets the related Bruton’s tyrosine kinase(BTK)with anIC₅₀value of 10.4 nM, but is more than 47-656-fold less potent against Blk,JAK3,EGFR,Itk, or Tec activity.

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

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 IC₅₀of 138 nM. BMX-IN-1 requires covalent modification of Cys⁴⁹⁶of BMX to achieve potent inhibition^[1].

524.59

Solid

C₂₉H₂₄N₄O₄S

1431525-23-3

Room temperature in continental US; may vary elsewhere.

DMF : 10 mg/mL(19.06 mM;Need ultrasonic)

DMSO : 8.33 mg/mL(15.88 mM;Need ultrasonic)

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