Biological Activity:

BI-7273 is a potent, selective and cell-permeable BRD9 inhibitor with IC50 ~19 nM (Alpha assay). It also inhibits BRD7 with IC50 ~117 nM (Alpha assay). It has high selectivity against the other bromodomain family members (48 bromodomains) and kinases. In EOL-1 cellular proliferation assay, BI-7273 has IC50 at 1400 nM. It has very good pharmacokinetic profiling. BI-7273 together with BI-9546, could be useful chemical tools to further explore BRD9 bromodomain biology in both in vitro and in vivo settings.

How to Use:

In vitro: BI-7273 was used at 1-10 µM in vitro and cellular assays.
In vivo: BI-7273 was orally dosed to mice at 180 mg/kg once per day.

Reference:

1. 1. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. (2016) J Med Chem. 59(10):4462-75.