BRPF Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S8265 GSK6853

GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.

Selective BRPF1, pIC50: 8.1
S5916 GSK 5959

GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.

Selective BRPF3, pIC50: 4.5; BRPF2, pIC50: 5.2; BRPF1, pIC50: 7.1
S7906 PFI-4

PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.

Selective BRPF3, IC50: >10μM; BRPF2, IC50: 7.9 μM; BRPF1, IC50: 80 nM
S7681 OF-1

OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.

Selective BRPF2, Kd: 500 nM; BRPF1B, Kd: 100 nM