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alpha-Mangostin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
alpha-Mangostin图片
CAS NO:6147-11-1
包装与价格:
包装价格(元)
Free Sample (0.1-0.5mg)电议
10mM (in 1mL DMSO)电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
alpha-Mangostin (α-Mangostin) 是具有广泛生物活性的膳食呫吨酮,如抗氧化剂,抗过敏,抗病毒,抗菌,抗炎和抗癌作用。它是IDH1突变体 (IDH1-R132H) 的抑制剂,Ki值为 2.85 μM。
Cas No.6147-11-1
别名α-倒捻子素; α-Mangostin
Canonical SMILESO=C1C2=C(OC3=C1C(C/C=C(C)\C)=C(OC)C(O)=C3)C=C(O)C(C/C=C(C)\C)=C2O
分子式C24H26O6
分子量410.46
溶解度DMSO: ≥ 37 mg/mL (90.14 mM)
储存条件Store at 2-8°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. IC50: 2.85 μM (IDH1-R132H)[1]

alpha-Mangostin (α-Mangostin) exhibits a selective inhibitory effect on IDH1-R132H, but not on IDH1. alpha-Mangostin (α-Mangostin) competitively inhibits the binding of alpha-mangostin (α-KG) to IDH1-R132H. The structure-relationship study reveals that alpha-Mangostin (α-Mangostin) exhibits the strongest core inhibitor structure. alpha-Mangostin (α-Mangostin) selectively promotes demethylation of 5-methylcytosine (5mC) and histone H3 trimethylated lysine residues in IDH1 (+/R132H) MCF10A cells[1]. Cell proliferation significantly decreases in a dose-dependent manner in the cells treated with alpha-mangostin. Alpha-mangostin also increases the levels of Bax (pro-apoptotic), cleaved caspase-3, cleaved caspase-9 and cleaved-poly(ADP-ribose) polymerase (PARP)[2]. alpha-Mangostin (α-Mangostin) significantly inhibits light-induced degeneration of photoreceptors and 200 μM H2O2-induced apoptosis of RPE cells. 200 μM H2O2-induced generation of reactive oxygen species (ROS) and light-induced generation of malondialdehyde (MDA) are suppressed by alpha-Mangostin (α-Mangostin)[3].

alpha-Mangostin (α-Mangostin) reduces risk of liver fibrosis through the decrease in p53 expression as compared to the TAA_DMSO treatment. The serum levels of the liver enzymes AST and ALT after treatment with α-mangostin decrease as compared to DMSO alone[4].

[1]. Kim HJ, et al. Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1. Bioorg Med Chem Lett. 2015 Dec 1;25(23):5625-31. [2]. Lee HN, et al. Antitumor and apoptosis-inducing effects of α-mangostin extracted from the pericarp of the mangosteen fruit (Garcinia mangostana L.) in YD-15 tongue mucoepidermoid carcinoma cells. Int J Mol Med. 2016 Apr;37(4):939-48.