• BET
  • p300/CBP
  • BRPF
  • bromodomain

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 BRPF1, pIC50: 7.1; BRPF2, pIC50: 5.2; BRPF3, pIC50: 4.5
S7906 PFI-4 PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. Selective BRPF1, IC50: 80 nM; BRPF2, IC50: 7.9 μM; BRPF3, IC50: >10μM
S7681 OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively. Selective BRPF1B, Kd: 100 nM; BRPF2, Kd: 500 nM