BRPF Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
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|
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|
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|
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|
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