银杏酸作用机制 - Medchemexpress - MCE中国

1、Product Data SheetGinkgolic AcidCat. No.: HY-N0077CAS No.: 22910-60-7分式: CHO分量: 346.5作靶点: E1/E2/E3 Enzyme作通路: Metabolic Enzyme/Protease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 : 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制备储备液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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实

3、验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.94 mM); Clear solution此案可获得 2.75 mg/mL (7.94 mM，饱和度未

4、知) 的澄清溶液。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.94 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.75 mg/mL (7.94 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取

5、 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Ginkgolic Acid种天然化合物， 在体外实验中抑制 SUMOylation 的 IC50 为3.0 M。体外研究 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.户使本产品发表的科研献 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