BI-7273

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC₅₀ and a K_d of 19 and 0.75 nM; also shows high effect on BRD7, with an IC₅₀ and a K_d of 117 nM and 0.3 nM. IC50 & Target: IC50: 19 nM (BRD9), 117 nM (BRD7)^[1]
Kd: 0.75 nM (BRD9), 0.3 nM (BRD7)^[1] In Vitro: BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC₅₀ and a K_d of 19 and 0.75 nM; also shows high effect on BRD7, with an IC₅₀ and a K_d of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with K_ds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC₅₀ of 1400 nM^[1].