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RGFP966 is a selective inhibitor of HDAC3 with IC50 value of 80 nM [1].

HDAC3 (histone deacetylase 3) is an isoform of HDACs family and plays an important role in DNA transcriptional regulation. It has been shown that HDACs involves in a variety of biologic processes, like DNA repair, replication, transcription and chromatin structure. Many studies have shown that HDACs is the most highly expressed class I HDAC in the brain and involves in learning and memory process negatively [2].

RGFP966 is a potent HDAC3 inhibitor and has no inhibition on other HDACs at the concentration up to 15 μM. Using a substrate-dependent biochemical assay to investigate RGFP966 inhibition of HDACs, and results showed that it inhibited HDAC3 with IC50 value of 80 nM while had no effective inhibition on other HDACs [1]. When tested with cutaneous T cell lymphoma (CTCL) cell lines with RGFP966, the cell growth were significantly decreased by inhibiting HDAC3 which increased cell apoptosis [3].

In male C57BL/6J mice model, trained them in object recognition (ORM) and location-dependent object recognition (OLM) with a subthreshold period after administration of RGFP966 significantly increased the novel object preference and enhanced enhanced long-term OLM in a dose-dependent manner [1].

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