|2-[(2-羟基萘-1-基亚甲基)氨基]-N-(1-苯乙基)苯甲酰胺|CsnPharm

CAS No.: 410536-97-9

Sirtinol/西丁醇 Catalog No. CSN12523

Synonyms: Sir Two Inhibitor Naphthol

Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Sirtuin 1

IC50:131μM Sirtuin 2

IC50:38μM
描述Sirtinol is a class III HDAC (Sirt1 and Sirt2) inhibitor with IC50 values of 38μM (measured by purified human hGST-SIRT2) and 131μM for Sirt2 and Sirt1, respectively, almost no activity on other HDACs. Treatment with sirtinol at concentration of 30μM and 120μM for 48h resulted a significant decrease in the growth and viability of all of the PCa cell lines while an increased acetylated FOXO1 in both the nuclear and cytosolic cellular fractions could be observed at 24h. Sirtinol at concentration of 100μM induced senescence-like growth arrest in MCF-7 and H1299 cells after 24-hour-treatment which may partially due to the impaired activation of Ras–MAPK pathway in response to EGF and IGF-I. Pretreatment with 3-20μM sirtinol 5 minutes before being activated with fMLF/CB could dose-dependently inhibited the activity of neutrophil elastase from human neutrophils in response to various stimulators. Intraperitoneal injection with sirtinol at dose of 2.5mg/kg or 5mg/kg significantly inhibited HNE-induced paw edema in mice. Also it attenuated the MAO activity (a marker of neutrophil infiltration) as well as reduced pulmonary wet/dry weight ratio in the LPS-induced ALI mouse model at dose of 5mg/kg.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human MCF7 cells	30 μM	Proliferation assay	24-72 h	Antiproliferative activity against human MCF7 cells at 30 uM after 24 to 72 hrs	24340169
human MCF7 cells	50 μM	Function assay	24 h	Inhibition of SIRT1 in human MCF7 cells assessed as increase in acetylation of p53 at lys 382 at 50 uM after 24 hrs by Western blot analysis	24340169
human U937 cells	50 μM	Apoptosis assay	45 h	Induction of apoptosis in human U937 cells at 50 uM after 45 hrs by flow cytometry	23189967

动物研究
剂量
Mice: 1 mg/kg^[3] (i.p.), 10 mg/kg^[4] (i.p.), 0.1 mg/kg - 0.5 mg/kg^[5] (i.p.) Rat: 1 mg/kg^[6] (i.v.); 10 mg/kg^[7] (i.p.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 1 mg/kg^[3] (i.p.), 10 mg/kg^[4] (i.p.), 0.1 mg/kg - 0.5 mg/kg^[5] (i.p.) Rat: 1 mg/kg^[6] (i.v.); 10 mg/kg^[7] (i.p.)
给药途径	i.p., i.v.

[1] Mai A, Massa S, et al. Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors. J Med Chem. 2005 Dec 1;48(24):7789-95.
[2] Grozinger CM, Chao ED, et al. Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening. J Biol Chem. 2001 Oct 19;276(42):38837-43.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5351 mL
- 12.6754 mL
- 25.3508 mL
- 5 mM
- 0.5070 mL
- 2.5351 mL
- 5.0702 mL
- 10 mM
- 0.2535 mL
- 1.2675 mL
- 2.5351 mL

技术信息

CAS号

410536-97-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H22N2O2

运输

蓝冰

分子量

394.47

别名

Sir Two Inhibitor Naphthol

溶解度

DMSO	23.0 mg/mL (58.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

0.4 mg/mL

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靶点	Description	IC50
Sirtuin 1		IC50:131μM
Sirtuin 2		IC50:38μM

Sirtinol/西丁醇 Catalog No. CSN12523

靶点选择性

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