alpha-Mangostin-α-Mangostin-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEalpha-MangostinCat. No.: HY-N0328CAS No.: 6147-11-1Synonyms: -Mangostin分式: CHO分量: 410.46作靶點(diǎn): Reactive Oxygen Species作通路: Immunology/Inflammation; Metabolic Enzyme/Protease; NF-B儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 37 mg/mL (90.14 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4363 mL 12.1815 mL 24.3629 mL5 mM 0.4873 mL 2.4363 mL 4.8726 mL10 mM 0.2436 mL 1.2181 mL 2.4363 mL請(qǐng)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(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL

3、 ACTIVITY物活性 alpha-Mangostin (-Mangostin)具有泛物活性的膳呫噸酮，如抗氧化劑，抗過敏，抗病毒，抗菌，抗炎和抗癌作。它是IDH1突變體 (IDH1-R132H) 的抑制劑，Ki值為 2.85 M。IC50 & Target IC50: 2.85 M (IDH1-R132H) 11/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 alpha-Mangostin (-Mangostin) exhibits a selective inhibitory effect on IDH1-R132H, but n

4、ot on IDH1. alpha-Mangostin (-Mangostin) competitively inhibits the binding of alpha-mangostin (-KG) to IDH1-R132H. Thestructurerelationship study reveals that alpha-Mangostin (-Mangostin) exhibits the strongest core inhibitorstructure. alpha-Mangostin (-Mangostin) selectively promotes demethylation

5、 of 5-methylcytosine (5mC) andhistone H3 trimethylated lysine residues in IDH1 (+/R132H) MCF10A cells 1. Cell proliferation significantlydecreases in a dose-dependent manner in the cells treated with alpha-mangostin. Alpha-mangostin alsoincreases the levels of Bax (pro-apoptotic), cleaved caspase-3,

6、 cleaved caspase-9 and cleaved-poly(ADP-ribose) polymerase (PARP) 2. alpha-Mangostin (-Mangostin) significantly inhibits light-induceddegeneration of photoreceptors and 200 M H2O2-induced apoptosis of RPE cells. 200 M H2O2-inducedgeneration of reactive oxygen species (ROS) and light-induced generati

7、on of malondialdehyde (MDA) aresuppressed by alpha-Mangostin (-Mangostin) 3.體內(nèi)研究 alpha-Mangostin (-Mangostin) reduces risk of liver fibrosis through the decrease in p53 expression ascompared to the TAA_DMSO treatment. The serum levels of the liver enzymes AST and ALT after treatmentwith -mangostin d

8、ecrease as compared to DMSO alone 4.PROTOCOLCell Assay 1 IDH1+/+ and IDH1 MCF10A cells are grown in DMEM/F-12 media, supplemented with 5% horse serum, 20ng/mL EGF, 0.5 g/mL hydrocortisone, 10 g/mL insulin. IDH1+/+ and IDH1 MCF10A cells are seeded in 6well plates. After an exposure to 5 M alpha-mango

9、stin. cells are collected after indicated times and theviable cell number is calculated, using hemacytometer counting 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Male Wistar rats are divided into 3 groups and treated with intraperiton

10、eal injections of TAA (200Administration 4 mg/kg). One subgroup is left untreated whereas the other two are treated either with 100 mg/kg alpha-mangostin or vehicle alone (80% DMSO, 20% water), which are administered intraperitoneally 3 times perweekfor a total of4 weeks. The incidence offibrotic no

11、dules on the liver and the serum levels of the liverenzymes aspartate transaminase (AST) and alanine transaminase (ALT) are measured 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kim HJ, et al. Discovery of -mangostin as a novel competi

12、tive inhibitor against mutant isocitrate dehydrogenase-1. Bioorg Med ChemLett. 2015 Dec 1;25(23):5625-31.2. Lee HN, et al. Antitumor and apoptosis-inducing effects of -mangostin extracted from the pericarp of the mangosteen fruit (Garciniamangostana L.) in YD-15 tongue mucoepidermoid carcinoma cells. Int J Mol Med. 2016 Apr;37(4):939-48.McePdfHeightCaution: