中文名称:
2-[[(2-羟基-1-萘基)亚甲基]氨基]-N-(1-苯基乙基)苯甲酰胺
中文同义词:
SIRTINOL, 去乙酰化酶;2-[[(2-羟基-1-萘基)亚甲基]氨基]-N-(1-苯基乙基)苯甲酰胺;去乙酰化酶;2-[(2-羟基萘-1-基亚甲基)氨基]-N-(1-苯乙基)苯甲酰胺;SIRTUIN抑制剂(SIRTINOL)
英文同义词:
{2-[(2-Hydroxynaphthalen-1-ylmethylene)amino]}-N-(1-phenethyl)benzamide (Sirtinol);2-[(2-HYDROXYNAPHTHALEN-1-YLMETHYLENE)AMINO]-N-(1-PHENETHYL)BENZAMIDE;SIRTINOL;SIR TWO INHIBITOR NAPHTHOL;(E)-2-((2-hydroxynaphthalen-1-yl)methyleneamino)-N-(1-phenylethyl)benzamide;2-[[(2-Hydroxy-1-naphthalenyl)methylene]amino]-N-(1-phenylethyl)benzamide;2-{[(2-hydroxynaphthalen-1-yl)Methylidene]aMino}-N-(2-phenylethyl)benzaMide;Sirtinol - CAS 410536-97-9 - Calbiochem
相关类别:
小分子抑制剂,天然产物;细胞生物学试剂;Inhibitors;Inhibitor;Other Enzyme Inhibitors.;Other enzyme inhibitors and activators
沸点
659.2±50.0 °C(Predicted)
酸度系数(pKa)
7.85±0.50(Predicted)
水溶解性
Soluble in water, DMSO and methanol
生物活性
Sirtinol 是 sirtuin (SIRT) 的抑制剂,对 ySir2,hSIRT2 和 hSIRT2 的 IC50 值分别为 48 μM,57.7 μM 和 131 μM。
靶点
ySir2
48 μM (IC 50 )
hSIRT2
57.7 μM (IC 50 )
hSIRT1
131 μM (IC 50 )
ySir2
48 μM (IC 50 )
hSIRT2
57.7 μM (IC 50 )
体外研究
Sirtinol reduces the growth of MCF-7 cells in a concentration- and time-dependent manner. The IC 50 values of sirtinol are 48.6 μM and 43.5 μM after 24 and 48 h of treatment, respectively. Sirtinol significantly decreases SIRT1 expression and increases the acetylated p53 level. Sirtinol attenuates the proliferation and induces apoptosis of nonsmall cell lung cancer (NSCLC) H1299 cells and causes the significantly increased level of FoxO3a, a proapoptotic transcription factor targeted by Sirt1.
体内研究
Sirtinol has anti-inflammatory effects through direct inhibition of HNE activity and attenuates HNE-induced and LPS-mediated tissue or organ injury.