銀杏酸作用機制 - Medchemexpress - MCE中國

1、Product Data SheetGinkgolic AcidCat. No.: HY-N0077CAS No.: 22910-60-7分式: CHO分量: 346.5作靶點: E1/E2/E3 Enzyme作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg/mL (288.60 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturatio

2、n unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.8860 mL 14.4300 mL 28.8600 mL5 mM 0.5772 mL 2.8860 mL 5.7720 mL10 mM 0.2886 mL 1.4430 mL 2.8860 mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實

3、驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.94 mM); Clear solution此案可獲得 2.75 mg/mL (7.94 mM，飽和度未

4、知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.94 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.75 mg/mL (7.94 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取

5、 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Ginkgolic Acid種天然化合物， 在體外實驗中抑制 SUMOylation 的 IC50 為3.0 M。體外研究 Ginkgolic acid inhibits the in vitro SUMOylation of RanGAP1-C2 with the IC50 values of 3.0 M. The level ofSUMOylated p53 is markedly reduced by the ginkgolic acid treatm

6、ent. Importantly, ginkgolic acid does not affectprotein ubiquitination in cells. Ginkgolic acid inhibits the binding between E1 and GA-BODIPY in a dose-dependentmanner1. Ginkgolic acid (31.2 g/mL) inhibits HIV protease activity by 60%, compared with the negative control, andthe effect is concentrati

7、on-dependent. Ginkgolic acid treatment (50 and 100 g/mL) effectively inhibits HIV infectionin human PBMC cells. Ginkgolic acid at the concentrations up to 150 g/mL does not cause any significantcytotoxicity in Jurkat cells2. GA only inhibits the growth of tumorogenic cell lines in a both dose- and t

8、ime-dependent manner. Tumor cells are treated with GA for 72 h, 70.534.54% Hep-2 and 63.57.2% Tca8113 cells areretarded at GO/G1 phase, and the percentage of apoptosis is 40.41.58 and 38.41.7%, respectively. GA-treatedactivated caspase-3 downregulates the expression of anti-apoptotic Bcl-2 protein a

9、nd upregulates the expression ofpro-apoptotic Bax protein, eventually leading to a decrease in the Bcl-2/Bax ratio in tumor cellsin human PBMC cells.Ginkgolic acid at the concentrations up to 150 g/mL does not cause any significant cytotoxicity in Jurkat cells3.PROTOCOLCell Assay 2 Jurkat cells (106

10、 cells/mL) are cultured in the RPMI medium with or without different concentrations of ginkgolic acidfor 48 hours to test the cytotoxicity of ginkgolic acid. The cytotoxicity of ginkgolic acid is determined using atetrazolium compound (MTS) and an electron coupling reagent (PMS). MTS is chemically r

11、educed by cells intoformazan, which is soluble in the tissue culture medium. The measurement of the absorbance of the formazan can becarried out using 96 well microplates at 492 nm. Since the production of formazan is proportional to the number ofliving cells, the intensity of the produced color is

12、a good indication of the viability of the cells.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻 Mol Ther Oncolytics. 2019 Dec 14;16:86-99. Toxicol Appl Pharmacol. 2018 Apr 15;345:1-9.See more customer validations on HYPERLINK www.MedChemE ww

13、w.MedChemEREFERENCES1. Fukuda I, et al. Ginkgolic acid inhibits protein SUMOylation by blocking formation of the E1-SUMO intermediate. Chem Biol. 2009 Feb 27;16(2):133-40.2. L JM, et al. Ginkgolic acid inhibits HIV protease activity and HIV infection in vitro. Med Sci Monit. 2012 Aug;18(8):BR293-298

14、.3. Zhou C, et al. Antitumor effects of ginkgolic acid in human cancer cell occur via cell cycle arrest and decrease the Bcl-2/Bax ratio to induce apoptosis.Chemotherapy. 2010;56(5):393-402.Page 2 of 3 www.MedChemE4. Qiu F, et al. Pharmacological inhibition of SUMO-1 with ginkgolic acid alleviates cardiac fibrosis induced by myocardial infarction in mice. Toxicol ApplPharmacol. 2018 Apr 15;345:1-9.McePdfH