MilliporeSigma™ Calbiochem™ BMX-IN-1

Description

• A cell-permeable tricyclic quinoline-acrylamide compound that potently inhibits BMX and BTK kinase activity (IC 50 = 8 and 10.4 nM, respectively) by covalently targeting ATP-binding site cysteine, while being less potent against TEC family kinases TEC, JAK3, BLK with the same conserved cysteine (IC 50 = 175, 377, and 653 nM, respectively)
• Only PI 3-Kγ/PIK3CG, SBK1, PIP5K2C (by ≥94% at 1μM), and TXK (by 75% at 1μM) are significantly inhibited by BMX-IN-1 in a selectivity profiling against 437 other kinase constructs
• Potently inhibits the proliferation of TEL-BMX transformed Ba/F3 Ba/F3 (GI 50 = 25nM), while being much less effective against TEL-BLK, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2E957D transformed Ba/F3 (GI 50 = ≥3.64μM) or a panel of 5 prostate cancer cell lines (GI 50 ≥2.46μM).