brpf2

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.

GSK9311 inhibits BRPF bromodomain (pIC50: 6.0 and 4.3 for BRPF1 and BRPF2, respectively). GSK9311 is a less active analog of GSK6853. It can be used as a negative control.

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.

OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain.

GSK9311 hydrochloride, a less active analog of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain (pIC50s: 6.0 and 4.3 for BRPF1 and BRPF2).

NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1 2 3=7.9 48 260 nM; Kds of BRPF1 2 3=40 210 940 nM). It also has excellent selectivity over nonclass IV BRD protei

GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.

BAY-299 is an effecitve inhibitor of the bromodomain and PHD finger family member BRPF2 and the TATA box binding protein-associated factors TAF1 and TAF1L with IC50s of 67 nM, 8 nM, and 106 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.

PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.