UBCS039 - Sirt6 Activator - 生命科學(xué)試劑 - 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 : 125 m

2、g/mL (505.48 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請根據(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，并請注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的?chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議

3、您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (8.41 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (8.41 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubili

4、ty: 2.08 mg/mL (8.41 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 UBCS039個(gè)合成的，SIRT6 的特異性激活劑，可在癌細(xì)胞中誘導(dǎo)噬，其EC50 值為38 M 1。IC50 & Target SIRT638 M (EC50)體外研究 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 您邊的抑制劑師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