| 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 |
