NI-57

NI-57 is an inhibitor of the bromodomains of BRPF proteins. The bromodomain and plant homeodomain finger-containing (BRPF) family are scaffolding proteins important for the recruitment and activation of MOZ/MORF histone acetyltransferases to chromatin. NI-57 binds to BRPF1B, BRPF2 and BRPF3 with Kd values of 31 nM, 108 nM and 408 nM respectively. It inhibits BRPF1 with an IC₅₀ of 114 nM. It shows functional activity in cellular assays by modulating the phenotype at low micromolar concentrations in cancer and inflammatory models.