SIRT1/2 INHIBITOR IV

中文名称:

SIRT1/2 INHIBITOR IV

中文同义词:

5-[(2-羟基萘-1-基)甲基]-6-苯基-2-硫代-2,3-二氢嘧啶-4(1H)-酮;SIRT1和SIRT1抑制剂(CAMBINOL);化合物CAMBINOL

英文名称:

NSC-1125476, Tetrahydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-Pyrimidinone, 5-(2-Hydroxynaphthalen-1-ylmethyl)-6-phenyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one, 5-[(2-hydroxy-1-naphthyl)methyl]-2-mercapto-6-phenyl-4(3H)-Pyrimidinone

英文同义词:

NSC-1125476;Tetrahydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-Pyrimidinone;SIRT1/2 Inhibitor IV, Cambinol;SIRT1/2 Inhibitor IV;CAMBINOL;NSC-1125476;Cambinol;NSC-1125476, Tetrahydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-Pyrimidinone, 5-(2-Hydroxynaphthalen-1-ylmethyl)-6-phenyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one, 5-[(2-hydroxy-1-naphthyl)methyl]-2-mercapto-6-phenyl-4(3H)-Pyrimidinone;5-(2-Hydroxynaphthalen-1-ylmethyl)-6-phenyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one

CAS号:

14513-15-6

分子式:

C21H16N2O2S

分子量:

360.43

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

14513-15-6.mol

熔点 

235 °C(dec.)

储存条件 

room temp

溶解度 

DMSO: ≥10mg/mL

形态

White solid

生物活性

Cambinol是一种新型的、非竞争性的nSMase2抑制剂，Ki值为7 μM。

靶点

Target Value nSMase2 (Cell-free assay) 7 μM(Ki)

Target

Value

nSMase2 (Cell-free assay)

7 μM(Ki)

体外研究

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.

体内研究

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.

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3