cecr2

NVS-CECR2-1 is a selective cat eye syndrome chromosome region candidate 2 (CECR2) inhibitor with antitumor activity and inhibits chromatin binding of CECR2 BRD. NVS-CECR2-1 is cytotoxic and can induce apoptosis.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd 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, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

GNE-375 is a selective and potent BRD9 inhibitor (IC50: 5 nM).GNE-375 inhibits BRD4, TAF1, and CECR2, and can be used to study epigenetic resistance.

BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A B over CECR2 and >100-fold selectivity over all other bromodomains.

TP-238, a potent and selective dual CECR2 BPTF probe, exhibits IC50 values of 30 nM and 350 nM, respectively. Additionally, it inhibits BRD9 with a pIC50 of 5.9, demonstrating lesser activity against another 338 kinases [1] [2].

TP-238 hydrochloride is a highly potent and selective dual CECR2 BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases.

GSK232 is a highly selective and cellularly penetrant inhibitor of CECR2 with outstanding physicochemical properties.

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2 4 9 and CECR2 (IC50: 0.41 0.29 0.122 0.017 μM), respectively.

BD-IN-1, a pan bromodomain (BD) inhibitor, exhibits K_D values of 250 nM for BRD4(1), 420 nM for CBP, 130 nM for BRPF1B, 430 nM for BRD7, 67 nM for BRD9, 240 nM for BRDT(1), and 970 nM for CECR2, respectively. This compound demonstrates antiproliferative activity [1].