Succinyl-phosphonate-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESuccinyl phosphonateCat. No.: HY-12688CAS No.: 26647-82-5分式: CHOP分量: 182.07作靶点: Others作通路: Others储存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 50 mg/mL (274.62 mM)* means soluble, but s

2、aturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 5.4924 mL 27.4620 mL 54.9239 mL5 mM 1.0985 mL 5.4924 mL 10.9848 mL10 mM 0.5492 mL 2.7462 mL 5.4924 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。BIOLOGICAL ACTIVITY物活性 Succinyl phosphonate-酮戊酸脱氢酶 (-ketoglutarate dehydrogenase) 的抑制剂

3、。体外研究Succinyl phosphonate is an -Ketoglutarate phosphoanalogue. It is found to be an effective inhibitor of -ketoglutarate oxidative decarboxylation, catalyzed by both muscle and bacterial -ketoglutaratedehydrogenase complexes, as well as muscle -ketoglutarate dehydrogenase 1. At a concentration of

4、0.01mM, succinyl phosphonate completely inhibits isolated brain KGDHC even in the presence of a 200-fold1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEhigher concentration of its substrate. In cultured human fibroblasts, 0.01 mM succinyl phosphonate produced70% inhibition of -ketoglutarate dehydro

5、genase complex. DESP and TESP are also inhibitory in the cellsystem, but only after preincubation, suggesting the release of their charged groups by cellular esterases 2.Succinyl phosphonate inhibits 2-Oxoglutarate dehydrogenase , the first rate-limiting component of themitochondrial multi-enzyme co

6、mplex of oxidative decarboxylation of 2-oxoglutarate, in a highly selective andefficient manner 3.PROTOCOLCell Assay 3 MTT assay is employed to test cellular viability. Serial dilutions of succinyl phosphonate (0.01-20 mM) areadded to cells in fresh culture media. During the medium exchange before t

7、he succinyl phosphonateaddition, glioblastoma cells are brought to DMEM with 1 g/L glucose, 1 mM pyruvate and 2 mM glutamax.The influence of succinyl phosphonate in minimal medium is studied in the earlier employed buffered saltsolution 3.MCE has not independently confirmed the accuracy of these met

8、hods. They are for reference only.户使本产品发表的科研献 Cancer Res. 2019 Jul 1;79(13):3281-3293. Free Radic Biol Med. 2016 Apr 9;96:22-33. Exp Cell Res. 2019 Jun 24. pii: S0014-4827(19)30324-6. Planta. 2018 Oct;248(4):963-979. Plant Signal Behav. 2019 Apr.See more customer validations on HYPERLINK / www.MedCh

9、emEREFERENCES1. Biryukov AI, et al. Succinyl phosphonate inhibits alpha-ketoglutarate oxidative decarboxylation, catalyzed by alpha-ketoglutaratedehydrogenase complexes from E. coli and pigeon breast muscle. FEBS Lett. 1996 Mar 11;382(1-2):167-70.2. Bunik VI, et al. Phosphonate analogues of alpha-ke

10、toglutarate inhibit the activity of the alpha-ketoglutaratedehydrogenase complexisolated from brain and in cultured cells. Biochemistry. 2005 Aug 9;44(31):10552-61.3. Bunik VI, et al. Inhibition of mitochondrial 2-oxoglutarate dehydrogenase impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Oncotarget. 2016 May 3;7(18):26400-21.McePdfHeightCaution: Product has not been fully v