Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetHistone Deacetylase

Cell permeable: yes

General description

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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Herman, D., et al. 2006. Nat. Chem. Biol.2, 551.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Harmful (C)