PF-CBP1 hydrochloride 是 CREB 结合蛋白溴结构域的一种高选择性抑制剂，抑制CREBBP和EP300溴结构域的IC50分别为 125 和 363 nM。它降低 LPS 诱导的巨噬细胞中炎症因子的表达，也可下调皮质神经元 RGS4 的表达，可用于癫痫和帕金森病等神经疾病的研究。

PF-CBP1 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.

PF-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[1].

2070014-93-4

C29H37ClN4O3

525.09

PF-CBP1 HCl

DMSO:100 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years