brd1

GSK-5959 is an effective, specific and cell permeable BRPF1 bromodomain inhibitor (IC50: ~80 nM). The selectivity of GSK-5959 for BRPF1 is >100-fold over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.

BRD1401 is a small molecule that targets the outer membrane protein OprH. It disrupts the interaction between OprH and LPS and can increase membrane fluidity.

BRD1652 is a highly selective and potent GSK3 inhibitor.

BRD1991 is a chemical compound that specifically disrupts the interaction between Beclin 1 and Bcl-2, thereby inducing autophagy. It accomplishes this without initiating apoptosis or other forms of cell death.

MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.

PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

BRPF1B/TRIM24-IN-1 (compound 34) is a potent inhibitor of TRIM24, BRPF1, and BRPF2, with IC50 values of 0.43 μM, 0.34 μM, and 1.75 μM respectively. The dissociation constants (KD) for its binding with the bromodomains of TRIM24, BRPF1, and BRD1 are 222 nM, 137 nM, and 1130 nM respectively.

NI-57 is an inhibitor of the bromodomain and plant homeodomain finger-containing (BRPF) family proteins, with IC50 values of 3.1 nM for BRPF1, 46 nM for BRPF2 (BRD1), and 140 nM for BRPF3.