PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).

CREBBP:125 nM, p300 BD:363 nM

PF-CBP1在原代巨噬细胞中调节关键炎症基因。PF-CBP1在神经元中下调RGS4，一个与帕金森病相关的靶点。在生化实验中，PF-CBP1对BRD4的选择性为139倍，通过ITC，选择性>105倍。PF-CBP1还是一种强效的EP300抑制剂，在巨噬细胞中没有细胞毒性。

Cells are pretreated with the probes PF-CBP1, ISOX-INACT, or ISOX-DUAL starting at 10 μM concentrations, and then serially diluted to 0.1 μM. After 30 min, the cells are treated with LPS to induce gene transcription and the expression levels of interleukin-6 (IL-6), IL-1β, and interferon-β (IFN-β)(which are known to be induced after 4 h of LPS exposure) are analyzed by RT-PCR. Probe PF-CBP1 moderately reduces LPS-induced IL-6 and IFN-β expression at 10 μM, and a decrease in IL-1β expression is evident at 3 μM.  (Only for Reference)