A cell-permeable pimeloylanilide compound that acts as a
FXN- (frataxin gene) specific HDAC (histone deacetylase) inhibitor. Reverses the silencing of
FXN transcription in FRDA (Friedreich′s ataxia) cells (~3-fold increase of
FXN mRNA at 5 μM in primary FRDA lymphocytes and ~3-fold frataxin expression in FRDA cell line at 2.5 μM) due to hypoacetylation of histones H3 and H4 by increasing acetylation at H3K14, H4K5 and H4K12, without significant changes in acetylation at H3K9, H4K8 and H4K16. In comparison, Trichostatin-A (Cat. No.
647925 and
647926) and SAHA, two other commonly used HDAC inhibitors, exhibit no effect on
FXN transcription.
