Cambinol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cambinol 是一种细胞渗透性 β-萘酚化合物，以底物竞争性而非 NAD 竞争性方式抑制 SIRT1/2 的 NAD 依赖性脱乙酰酶活性（IC50 分别为 56/59 μM）。

Cambinol is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1/2 (IC50: 56/59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Cambinol inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 μM) and no inhibitory for the class I and II HDACs. In BCL6-expressing Burkitt lymphoma cell lines, Cambinol-induced apoptosis has been attributed to the hyperacetylation of p53 and BCL6.

Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induces apoptosis, which is accompanied by hyperacetylation of BCL6 and p53. Cambinol has only weak inhibitory activity against SIRT5 (42% inhibition at 300 μM) and no activity against SIRT3.

Cambinol is well tolerated in mice (100 mg/kg) and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss occurs in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents.

SIRT 1/2 inhibitor IV | NSC112546 | NSC-112546

Metabolic Enzyme/Protease

P450

SIRT1| SIRT2

——

——

14513-15-6

360.09

C21H16N2O2S

>98% (HPLC)

DMSO : 50 mg/mL. 138.72 mM;H2O : < 0.1 mg/mL

O=c1c(Cc2c3ccccc3ccc2O)c(c2ccccc2)[nH]c(=S)[nH]1

5-((2-hydroxynaphthalen-1-yl)methyl)-6-phenyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one

(-20℃)

With Ice Pack

≥ 2 years