Sirtinol - Sirtuin 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESirtinolCat. No.: HY-13515CAS No.: 410536-97-9分式: CHNO分量: 394.47作靶點(diǎn): Sirtuin; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6.5

2、mg/mL (16.48 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5350 mL 12.6752 mL 25.3505 mL5 mM 0.5070 mL 2.5350 mL 5.0701 mL10 mM 0.2535 mL 1.2675 mL 2.5350 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Sirtinol是sirtuin 的抑制劑，對(duì) ySir2，hSIRT2 和 hSIRT2 的 I

3、C50 值分別為 48 M，57.7 M 和 131 M。IC50 & Target ySir2 hSIRT2 hSIRT148 M (IC50) 57.7 M (IC50) 131 M (IC50)體外研究Sirtinol reduces the growth of MCF-7 cells in a concentration- and time-dependent manner. The IC50 valuesof sirtinol are 48.6 M and 43.5 M after 24 and 48 h of treatment, respectively. Sirtinol si

4、gnificantly1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEdecreases SIRT1 expression and increases the acetylated p53 level 1. Sirtinol attenuates the proliferationand induces apoptosis of nonsmall cell lung cancer (NSCLC) H1299 cells and causes the significantlyincreased level of FoxO3a, a proapo

5、ptotic transcription factor targeted by Sirt1 2.體內(nèi)研究 Sirtinol has anti-inflammatory effects through direct inhibition of HNE activity and attenuates HNE-inducedand LPS-mediated tissue or organ injury 3.PROTOCOLCell Assay 2 Sirtinol is dissolved in 100% DMSO at concentration of 10mM and stored at 20C

6、 until use. The cellproliferation of H1299 cells is determined by trypan blue dye exclusion assay. Human nonsmall cell lungcancer (NSCLC) cells are seeded in 12-well plates and treated with indicated concentrations of sirtinol (0, 10,20, and 50M) for 24h and 48h, respectively. After incubation, the

7、cells are stained by 0.2% trypan blue andcounted by Countess 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: 30 male mice (2025 g, 78 weeks old) are used in this model. Briefly, mice are randomly divided intoAdministration 3 five groups;

8、then mice are intraperitoneally injected with 50 L DMSO (vehicle group) or sirtinol (2.5 or 5.0mg/kg body weight). After 1 h, paw inflammation is induced . The thickness of the paw is measured beforeand after HNE or saline injection 3.MCE has not independently confirmed the accuracy of these methods

9、. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Death Dis. 2018 May 1;9(5):559. Mol Cell Biochem. 2018 Feb;439(1-2):213-223.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wang J, et al. Sirtinol, a class III HDAC inhibitor, induces apoptotic and autophagic cell death in MCF-7 h

10、uman breast cancer cells. Int JOncol. 2012 Sep;41(3):1101-1109.2. Fong Y, et al. The antiproliferative and apoptotic effects of sirtinol, a sirtuin inhibitor on human lung cancer cells by modulating Akt/-catenin-Foxo3a axis. ScientificWorldJournal. 2014;2014:937051.3. Tsai YF, et al. Sirtinol inhibi

11、ts neutrophil elastase activity and attenuates lipopolysaccharide-mediated acute lung injury in mice. Sci Rep.2015 Feb 10;5:8347.4. Mai A, 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.McePdfHeightCaution: Product has not