Description: I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3. Target: Epigenetic Reader Domain. Smiles: CCn1cc(-c2cccc(c2)C(F)(F)F)c2sc(cc2c1=O)C(=N)NC1CCS(=O)(=O)CC1. References: Theodoulou NH, et al. J Med Chem. 2016, 59(4):1425-1439.

BRD9 contains a single bromodomain and has five isoforms that are produced by alternative splicing. It is thought to function in chromatin remodeling as part of the SWI/SNF complex. I-BRD9 is a BRD9 bromodomain inhibitor with a pIC50 value of 7.3 and a pKd value of 8.7. It displays 700-fold greater selectivity over...

BET bromodomain inhibitor with Kd values of 160, 170, 380, 490, 830 and 850nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2), respectively. XD14 also inhibits BRDT(1), CBP, p300 and BRDT(2) with Kd values of 1.2, 1.6, 2.6 and 3.7µM, respectively. XD14 has shown to attenuate proliferation of HL-60...

I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 has a pIC50 value of 7.3 for BRD9 inhibitor, with greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is also shows a greater...