BMX-IN-1 是 X 染色体上的骨髓酪氨酸激酶 (BMX, IC50 = 8 nM) 和相关的布鲁顿酪氨酸激酶 (BTK, IC50 = 10.4 nM) 的特异性抑制剂，但 BMX-IN-1 对 Blk、JAK3、EGFR、Itk 或 Tec 活性的效力要低 47-656 倍以上。

BMX-IN-1 is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton’s tyrosine kinase (BTK, IC50 = 10.4 nM), but BMX-IN-1 is more than 47-656 fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

BMX-IN-1 inhibits only wild-type BMX with an IC50 of 138 nM. 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[1].

1431525-23-3

C29H24N4O4S

524.59

BMX kinase inhibitor

DMF:9 mg/mL (17.16 mM),Need ultrasonic
DMSO:8 mg/mL (15.25 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years