DESCRIPTION RGFP966 is a selective inhibitor of histone deacetylase 3 (HDAC3) . In rodent studies, RGFP966-induced inhibition of HDAC3 appears to enhance memory processes involved in extinction of drug-seeking behaviour . (GtoPdb)

COMMENT This is an N-(o-amino-phenyl)carboxamide HDAC3-selective inhibitor with an IC50 of 80 nM and 'no effective inhibition of other HDACs' at concentrations up to 15 uM utilizing a substrate-dependent biochemical assay with recombinant human protein (Malvaez et al PNAS 2013; 110: 2647-2652 - primary data not shown). However, functional data suggests possible inhibition of other class I HDACs at concentrations >1 uM (Matthews et al Blood 2015; 126: 2392-2403) - please refer to 'cellular concentration notes'. For in vivo dosing, 10 mg/kg delivered subcutaneously achieves a maximum tissue concentration (brain) in mice of 3.15 uM at 30 minutes, with concentrations exceeding the IC50 for HDAC3 for at least 2 hours in this tissue. Jun 1 2017 - 1:56pm; RGFP966 has been demonstrated to have selective activity for HDAC3 in biochemical assays over most other HDAC enzymes. In cells, Matthews et al., (Blood, 2015) observed that RGFP966 treatment phenocopied genetic HDAC3 perturbation up to ~1,000 nM. Thus, cellular studies using RGFP966 for selective pharmacologic HDAC3 perturbation should be limited to concentrations <1,000 nM. In mouse and rat models, RGFP966 has been observed to be brain-penetrant when dosed subcutaneously. When used for in vivo studies, care should be taken to pair phenotypic observations from genetic-perturbation studies of HDACs in order to have higher confidence in HDAC3-selective effects. Jun 13 2017 - 2:11pm

DESCRIPTION RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 ¦ÌM. RGFP966 can penetrate the blood brain barrier (BBB).

DESCRIPTION (E,E)-RGFP966 is a selective and CNS permeable HDAC3 inhibitor that can be used for the research of Huntington¡¯s disease[1].

PRICE 90

DESCRIPTION RGFP966 is an HDAC3 inhibitor (IC50: 0.08 ??M) and does not affect other HDACs at concentrations up to 15 ??M.

PRICE 38

DESCRIPTION RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 ??M, exhibits > 200-fold selectivity over other HDAC.

MOA Inhibitor (Chemical Probes.org)

DESCRIPTION Potent, selective and irreversible alpha/beta-hydrolase domain 6 (ABHD6) inhibitor (Tocris Bioactive Compound Library)

DESCRIPTION RGFP966 is a selective HDAC3 inhibitor. Systemic treatment with RGFP966 facilitates extinction in mice in a manner resistant to reinstatement. A single treatment of RGFP966 enhances extinction of a previously established cocaine-conditioned place preference, while simultaneously enhancing long-term object-location memory within subjects. During extinction consolidation, HDAC3 inhibition promotes a distinct pattern of histone acetylation linked to gene expression within the infralimbic cortex, hippocampus, and nucleus accumbens. Thus, the facilitated extinction of drug-seeking cannot be explained by adverse effects on performance. These results demonstrate that HDAC3 inhibition enhances the memory processes involved in extinction of drug-seeking behavior. (BOC Sciences Bioactive Compounds)

DESCRIPTION RGFP966 is an HDAC3 inhibitor (IC50: 0.08 μM) and does not affect other HDACs at concentrations up to 15 μM. (TargetMol Bioactive Compound Library)