MilliporeSigma™ Calbiochem™ BMX-IN-1

Description

A cell-permeable tricyclic quinoline-acrylamide compound that potently inhibits BMX and BTK kinase activity (IC₅₀ = 8 and

A cell-permeable tricyclic quinoline-acrylamide compound that potently inhibits BMX and BTK kinase activity (IC₅₀ = 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 (IC₅₀ = 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 (GI₅₀ = 25nM), while being much less effective against TEL-BLK, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2E957D transformed Ba/F3 (GI₅₀ = ≥3.64μM) or a panel of 5 prostate cancer cell lines (GI₅₀ ≥2.46μM).

Specifications

• Color: Off-white
• Description: 95% by HPLC
• Target Proteins: BMX
• Molecular Formula: C₂₉H₂₄N₄O₄S
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 10 mg