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Background
RG2833 is a histone deacetylase (HDAC) inhibitor. In the neuronal cell, RG2833 increased Friedreich Ataxia (FXN) mRNA and protein levels, with concomitant changes in the epigenetic state of the gene. In PBMCs, RG2833 inhibited HDAC expression and increased H3K9 acetylation, and increased FXN mRNA in blood from patients.In iPSC-derived neuronal cell model, plasma RG2833 (5μM) inhibited maximal deacetylase and upregulated FXN. The result showed a good correlation between increase in FXN transcript and inhibition of deacetylase activity, providing evidence that the mechanism of action of RG2833 is through deacetylation. [1]
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