GXH-II-052 is a potent bivalent inhibitor targeting the bromodomain and extraterminal domain (BET). It exhibits significant binding affinity to various BET proteins, including BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, and BRDT-T, with dissociation constants (Kd) of 28, 9.1, 4.8, 0.6, 8.4, and 2.6 nM, respectively. Additionally, GXH-II-052 demonstrates antiproliferative effects and reduces the expression of c-Myc [1].

BRD4(2):9.1 nM (Kd), BRDT (1):0.6 nM (Kd), BRD4-T:4.8 nM (Kd), BRD41:28 nM (Kd), BRDT-T:2.6 nM (Kd), BRDT2:8.4 nM (Kd)