3031654-46-0

NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc[1].

BRD4-1: 0.095 nM (Kd); BRD4-2: 0.032 nM (Kd); BRD4-T: 0.29 nM (Kd); BRDT-1: 0.089 nM (Kd); BRDT-2: 5.5 nM (Kd); BRDT-T: 0.058 nM (Kd)

[1] Guan X, et al. Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity. J Med Chem. 2022 Jul 22. DOI:10.1021/acs.jmedchem.2c00453