RGFP966

Description	RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC. 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. HDAC3 inhibition using a first in class selective inhibitor, RGFP966, resulted in decreased cell growth in CTCL cell lines due to increased apoptosis that was associated with DNA damage and impaired S phase progression. Selective inhibition of HDAC3 could be useful in treatment of CTCL by disrupting DNA replication of the rapidly cycling tumor cells, ultimately leading to cell death.
Pathways	Cell Cycle/DNA Damage Epigenetics
Targets	HDAC

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