RGFP963, or RGFP-963, is a histone deacetylase (HDAC) inhibitor which is used in scientific research. It is a selective class I HDAC inhibitor, including of HDAC1, HDAC2, and HDAC3 (IC50Tooltip half-maximal inhibitory concentration = 1,510 nM, 750 nM, and 96 nM, respectively). The drug also weakly inhibits HDAC10 (IC50 = 6,640–10,000 nM), whereas it showed no inhibition of other HDACs at a concentration of up to 20,000 nM. RGFP963 enhances the consolidation of cued fear extinction in rodents, with this thought to be mediated by inhibition of HDAC1 and/or HDAC2 and not by inhibition of HDAC3. In addition, the drug promotes synaptogenesis in vitro and enhances memory in an animal model of Alzheimer's disease in rodents. It also enhanced cognition in a model of amyotrophic lateral sclerosis (ALS) in rodents. The pharmacokinetics of RGFP963 have been studied and it is brain-penetrant in rodents. RGFP963 was first described in the scientific literature by 2015.
See also Histone deacetylase inhibitor RGFP136 RGFP966
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