SIRT1 Inhibitor III

A cell-permeable indole compound that acts as a potent and highly selective inhibitor of SIRT1 (IC₅₀ = 98 nM). It inhibits other sirtuin family deacetylases only at much higher concentrations (IC₅₀ = 19.6 and 48.7 µM for SIRT2 and SIRT3, respectively) and shows no inhibitory effect against class I and II HDACs or NAD glycohydrolase even at concentrations as high as 100 µM. Shown to be orally bioavailable with a serum half-life of 136 minutes in mice in vivo.

Primary Target
SIRT1

Target IC₅₀: 98 nM against SIRT1

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

Solomon, J.M., et al. 2006. Mol. Cell. Biol.26, 28.
Napper, A.D., et al. 2005. J. Med. Chem.48, 8045.

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

Toxicity: Irritant (B)