SIRT1/2 Inhibitor IV; Cambinol

Biochem/physiol Actions

Primary TargethSIRT1 and hSIRT2

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 56 µM and 59 µM against the NAD-dependent deacetylase activity of hSIRT1 and hSIRT2, respectively

Cell permeable: yes

General description

A cell-permeable β-naphthol compound that inhibits the NAD-dependent deacetylase activity of hSIRT1 and hSIRT2 (IC₅₀ = 56 µM and 59 µM, respectively) in a substrate-, but not NAD-, competitive manner. It inhibits SIRT5 deacetylase activity only at much higher concentrations (IC₅₀ >300 µM) and exhibits no inhibition against class I and II HDACs. Cambinol-induced apoptosis in BCL6-expressing Burkitt lymphoma cell lines has been attributed to the hyperacetylation of BCL6 and p53. Shown to effectively inhibit xenografted Daudi Burkitt lymphoma growth in mice in vivo.

Legal Information

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

Other Notes

Heltweg, B., et al. 2006. Cancer Res.66, 4368.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Irritant (B)