2016年12月28日星期三

BI-9564|BI9564|BRD9/7 inhibitor

BI-9564|BI9564|BRD9/7 inhibitor

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.

Product Name: BI-9564|Cat No: DC9888|cas: 1883429-22-8|Other Names: BI9564,BI 9564

BI-9564 (MW 353.4) is a BRD9 / 7 specific inhibitor that has been developed in collaboration with Boehringer Ingelheim. This probe was discovered through fragment-based screening and optimized by structure guided design. BI-9564 binds to BRD9 with a higher affinity (Kd=14 nM, ITC) than to BRD7 (Kd=239nM, ITC), is completely negative on BET family members (>100 µM by AlphaScreen) and demonstrates cellular activity by FRAP on BRD9 and BRD7 at 0.1 µM and 1 µM, respectively. BI-9564 shows off-target selectivity to CECR2 in vitro (258 nM, ITC), but not in cells (at 1 µM, FRAP).

For the research and scientific use only, not for human use!

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