General description
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.
Biochem/physiol Actions
Primary Target
SIRT1
Target IC50: 98 nM against SIRT1
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Solomon, J.M., et al. 2006. Mol. Cell. Biol.26, 28.
Napper, A.D., et al. 2005. J. Med. Chem.48, 8045.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 566322-5MG
- CAS:
- 49843-98-3