UBCS039 - Sirt6 Activator - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUBCS039Cat. No.: HY-115453CAS No.: 358721-70-7分式: CHN分量: 247.29作靶点: Sirtuin; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 m

2、g/mL (505.48 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.0438 mL 20.2192 mL 40.4384 mL5 mM 0.8088 mL 4.0438 mL 8.0877 mL10 mM 0.4044 mL 2.0219 mL 4.0438 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议

3、您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (8.41 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (8.41 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubili

4、ty: 2.08 mg/mL (8.41 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 UBCS039个合成的，SIRT6 的特异性激活剂，可在癌细胞中诱导噬，其EC50 值为38 M 1。IC50 & Target SIRT638 M (EC50)体外研究 UBCS039 (75 M, 48 or 72 hours) induces deacetylation of SIRT6-targeted histone H3 sites in humancancer

5、 cells 2.UBCS039 leads to autophagosome accumulation in human cancer cells 2.UBCS039 induces autophagy via AMP-activated protein kinase (AMPK) signaling pathway activation 2.Western Blot Analysis 2Cell Line: Human H1299 cells.Concentration: 75 M.Incubation Time: 48 and 72 hours.Result: Induced deace

6、tylation of SIRT6-targeted histone H3 sites in human H1299 cells.Western Blot Analysis 2Cell Line: Human H1299 cells.Concentration: 75 M.Incubation Time: 48 and 72 hours.Result: Induced deacetylation of SIRT6-targeted histone H3 sites in human H1299 cells.Cell Proliferation Assay 2Cell Line: Human H

7、1299 cells.Concentration: 100 M.Incubation Time: 48 and 72 hours.Result: Led to a strong decrease of cell proliferation in a dose-dependent manner whencompared with control or DMSO-treated cells, starting from day 3 of growth (48 h aftertreatment) in both H1299 and HeLa cell lines.REFERENCES1. Weiji

8、e You, et al. Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules. Angew. Chem. Int. Ed. 2017, 56, 1007-1011.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. Sara Iachettini, et al. Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells. Cell Death and Disease(2018) 9:996.McePdfHeightCaution: Product has not been fully validated for medical application