Biological Activity:

PF-CBP1 is a potent and selective CBP/p300 bromodomain inhibitor (IC50 ~125 nM for CBP and 363 nM for p300). It has >100-fold selectivity for CBP over BRD4, and shows selectivity over a panel of other bromodomains. PF-CBP1 reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. It can also downregulate RGS4 expression in primary cortical neurons in vitro.

How to Use:

In vitro: PF-CBP1 was used at 10 µM final concentration in various assays.
In vivo: n/a

Reference:

1. 1. Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. (2015) Chem Biol. 22(12):1588-96.