CECR2 Inhibitor

NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC₅₀=47 nM; K_D=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism. NVS-CECR2-1 is a chemical probe.

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d of 2.2 nM and an IC₅₀ of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.

TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC₅₀ values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC₅₀ of 5.9 and is less active against other 338 kinases.

TP-238 is a potent and selective dual CECR2/BPTF probe with IC₅₀ values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC₅₀ of 5.9 and is less active against other 338 kinases.