產品屬性：

Cas No.: 6147-11-1

別名: N/A

化學名: N/A

分子式: C24H26O6

分子量: 410.46

溶解度: DMSO: ≥ 37 mg/mL (90.14 mM)

儲存條件: 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

產品描述：

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.
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