+ Enzyme (nM) HDAC1 1,510 HDAC2 750 HDAC3 96 HDAC4 >20,000 HDAC5 >20,000 HDAC6 >20,000 HDAC7 >20,000 HDAC8 >20,000 HDAC9 >20,000 HDAC10 6,640–10,000 HDAC11 27,700 Refs:
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 ( = 1,510nM, 750nM, and 96nM, respectively). The drug also weakly inhibits HDAC10 ( = 6,640–10,000nM), whereas it showed no inhibition of other HDACs at a concentration of up to 20,000nM. 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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