表观遗传阅读器域抑制剂;Epigenetic Reader Domain Inhibitors;;InformationPF-CBP1 HCl PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP) .It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.TargetsCREBBP (Cell-free assay); p300/CBP (Cell-free assay) 125nM; 363nMIn vitroPF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 down regulates RGS4 in neurons, a target linked to Parkinson\'s disease.It is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC.PF-CBP1 is also a potent inhibitor of EP300 and possesses no cytotoxicity in macrophages, and hepatotoxicity in cell-based models as long as the concentration is not very high.Cell Research(from reference)Cell lines:mouse J774 macrophage-like cell line Concentrations:0.1-10\xa0μM Incubation Time:30min