Description: BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 µM. Target: Epigenetic Reader Domain. Smiles: COc1cc(c(OC)cc1CN(C)C)-c1cn(C)c(=O)c2cnccc12. References: Martin LJ, et al. J Med Chem. 2016, 59(10):4462-75.

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM, IC50s = 75 nM and 3.4 µM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 µM and 1 µM, respectively. It does not bind to other bromodomain-containing...

BI-9564 inhibits BRD9 and BRD7 bromodomains and exhibits no significant off-target pharmacology against a panel of 324 kinases and 55 GPCRs at concentrations less than 5 µM. BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM, IC50s = 75 nM and 3.4 µM, respectively) that...