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MilliporeSigma™ Calbiochem™ BMX-IN-1

Catalog No. 5050210001 Shop All MilliporeSigma Products
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50-502-10001 10 mg
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Catalog No. 50-502-10001 Supplier MilliporeSigma™ Supplier No. 5050210001
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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).
TRUSTED_SUSTAINABILITY

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
Product Title
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