Biochem/physiol Actions

Primary TargetySir2

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 48 µM, 131 µM and 58 µM for ySir2, hSIRT1 and hSIRT2, respectively

Cell permeable: yes

General description

A cell-permeable 2-hydroxy-1-napthaldehyde derivative that acts as a specific and a direct inhibitor of sirtuin class of histone deacetylase (HDAC) activity. Does not affect human HDAC1. Reported to block Sir2p transcriptional silencing activity in vivo (IC₅₀ = 25 µM) and NAD-dependent HDAC activity in purified recombinant yeast Sir2p and human SIRT2 in vitro (IC₅₀ = 68 µM and 38 µM, respectively).

Legal Information

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

Other Notes

Mai, A., et al. 2005. J. Med. Chem.48, 7789.Grozinger, C.M., et al. 2001. J. Biol. Chem.276, 38837.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

A 10 mM (1 mg/254 µl) solution of Sirtinol (Cat. No. 566320) in DMSO.

Reconstitution

Following initial thaw, aliquot and refrigerate (4°C).

Warning

Toxicity: Irritant (B)