別名

SIRT1/2 Inhibitor IV, Cambinol,5-(2-Hydroxy-naphthalen-1-ylmethyl)-6-phenyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one, NSC-112546, SIRT1 Inhibitor II, SIRT2 Inhibitor VI

一般描述

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.

生化/生理作用

Cell permeable: yes Primary Target
hSIRT1 and hSIRT2 Product does not compete with ATP. Reversible: no Target IC50: 56 μM and 59 μM against the NAD-dependent deacetylase activity of hSIRT1 and hSIRT2, respectively

重懸

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