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Sirtinol

现货
Catalog No.
A4183
SIRT抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 610.00
现货
5mg
¥ 500.00
现货
25mg
¥ 1,900.00
现货

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Background

Sirtinol is an inhibitor of SIRT with IC50 value of 48.6 μM (24 h) and 43.5 μM (48 h) in MCF-7 cells [1].

Sirtinol significantly reduces the growth of MCF-7 cells in a concentration- and time-dependent manner. Meanwhile, the expression level of SIRT1 is notably decreased by sirtinol results in an induction of acetylated p53. It is found that sirtinol decreases the the expression of cell cycle-regulated proteins such as cyclin B1, cyclin D1, CDK2 and CDK6 and subsequently induces G1 phase arrest which indicates cell apoptosis. Furthermore, sirtinol is also demonstrated to induce autophagy in MCF-7 cells. Other in vitro assays show that sirtinol inhibits SIRT2 (amino acids 18–340) with IC50 value of 45 μM while it does not inhibit HDAC1 at 50 and 100 μM [1, 2].

Reference:
[1] Wang J, Kim TH, Ahn MY, Lee J, Jung JH, Choi WS, Lee BM, Yoon KS, Yoon S, Kim HS.  Sirtinol, a class III HDAC inhibitor, induces apoptotic and autophagic cell death in MCF-7 human breast cancer cells. Int J Oncol. 2012 Sep;41(3):1101-9.
[2] Grozinger CM, Chao ED, Blackwell HE, Moazed D, Schreiber SL.  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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt394.47
Cas No.410536-97-9
FormulaC26H22N2O2
Solubility≥19.7 mg/mL in DMSO, <2.32 mg/mL in EtOH, <2.23 mg/mL in H2O
Chemical Name2-[[(Z)-(2-oxonaphthalen-1-ylidene)methyl]amino]-N-(1-phenylethyl)benzamide
SDFDownload SDF
Canonical SMILESCC(C1=CC=CC=C1)NC(=O)C2=CC=CC=C2NC=C3C(=O)C=CC4=CC=CC=C43
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

人源Sirt2酶体外活性抑制实验

将1.5 μg重组蛋白GST-Sirt2(氨基酸18 ~ 340)置于50 μL实验缓冲液(50 mM Tris-HCl,pH 8.8,4 mM MgCl2,0.2 mM二硫苏糖醇,不同浓度的Sirtinol,50 μM NAD,以及通过酸萃取法得到的氚标记的乙酰化HeLa细胞组蛋白 (1000 cpm))中,于30 °C下,孵育2小时。通过闪烁计数检测可溶于乙酸乙酯的[3H]乙酸,测定HDAC活性。

细胞实验 [2]:

细胞系

LNCaP、22Rv1、DU145和PC3细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

30或120 μM;24或48小时

实验结果

给予Sirtinol(30和120 μM)。于24或48小时后,Sirtinol显著降低所有PCa细胞系的生长与存活能力。

动物实验 [3]:

动物模型

雄性SD大鼠创伤出血模型

给药剂量

1 mg/kg;静脉注射

实验结果

在雄性SD大鼠创伤出血模型中,Sirtinol (1 mg/kg) 减少促炎细胞因子的产生并防止肝损伤。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Grozinger CM, Chao ED, Blackwell HE, Moazed D, Schreiber SL. 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.

[2]. Jung-Hynes B, Nihal M, Zhong W, Ahmad N. Role of sirtuin histone deacetylase SIRT1 in prostate cancer. A target for prostate cancer management via its inhibition? J Biol Chem. 2009 Feb 6;284(6):3823-32.

[3]. Liu FC, Day YJ, Liou JT, Lau YT, Yu HP. Sirtinol attenuates hepatic injury and pro-inflammatory cytokine production following trauma-hemorrhage in male Sprague-Dawley rats. Acta Anaesthesiol Scand. 2008 May;52(5):635-40.

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