BI-9564

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (K_ds = 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.^1,2 It does not bind to other bromodomain-containing BET family members (IC₅₀s >100 µM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (K_d = 258 nM), but not in cell-based assays at concentrations up to 1 µM.¹ BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC₅₀ = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day).¹ See the Structural Genomics Consortium (SGC) website for more information.

WARNING This product is not for human or veterinary use.

1. Martin, L.J., Koegl, M., Bader, G., et al. Structure-based design of an in vivo active selective BRD9 inhibitor. J. Med. Chem. 59(10), 4462-4475 (2016).

2. Karim, R.M., and Schönbrunn, E. An advanced tool to interrogate BRD9. J. Med. Chem. 59(10), 4459-4461 (2016).