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.

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

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.

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

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.

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).

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