| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Mutant IDH1 (IDH1-R132H); human STING (Stimulator of Interferon Genes); COX-2. Alpha-Mangostin competitively inhibits the binding of α-KG to IDH1-R132H with a Ki of 2.85 µM. It is a potent agonist of human STING, inducing IFN-β production. It also inhibits COX-2 activity.
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| ln Vitro |
α-Mangostin (α-Mangostin) inhibits IDH1-R132H, but not IDH1. IDH1-R132H is inhibited by α-Mangostin. Structure: Research has indicated that the strongest core flipped structure is found in α-Mangostin (α-Mangostin). In IDH1 (+/R132H) MCF10A cells, α-Mangostin (α-Mangostin) preferentially inhibits the demethylation of 5-methylcellulose (5mC) and histone H3 trimethylated lysine residues [1]. Cell proliferation was considerably inhibited in a dose-dependent manner in cells treated with α-mangostin. Additionally, Bax (pigmentogen), mitochondrial caspase-3, mitochondrial caspase-9, and mitochondrial poly(ADP-ribose) polymerase (PARP) are all upregulated by α-mangosteen [2]. α-Mangostin (α-Mangostin) notably reduces photoThe production of reactive oxygen species (ROS) and malondialdehyde (MDA) produced by light is inhibited by α-Mangostin (α-Mangostin) at 200 μM H2O2[3].
Alpha-Mangostin demonstrates potent in vitro activity against various targets. It inhibits mutant IDH1-R132H with a Ki of 2.85 µM. It is a human STING agonist that induces IFN-β production and repolarizes human monocyte-derived M2 macrophages to M1. It inhibits proliferation and induces apoptosis selectively in pancreatic cancer stem cells and cancer cell lines. It also exhibits antibacterial, antifungal, and antimalarial activities. |
| ln Vivo |
α-Mangostin (α-Mangostin) lowers the incidence of liver fibrosis by lowering p53 expression compared with TAA_DMSO therapy. Serum levels of liver enzymes AST and ALT were lowered after α-Mangostin therapy compared with DMSO alone [4] .
In vivo, Alpha-Mangostin has been shown to suppress light-induced degeneration of photoreceptors and H2O2-induced apoptosis of RPE cells. It reduces the risk of liver fibrosis through decreased p53 expression. It has protective effects on kidney, heart, and brain tissues against oxidative stress. Serum levels of liver enzymes AST and ALT decrease after treatment. |
| Enzyme Assay |
In vitro enzyme inhibition assays for Alpha-Mangostin are performed using recombinant IDH1-R132H enzyme. The enzyme is incubated with α-KG substrate and varying concentrations of Alpha-Mangostin. The production of 2-hydroxyglutarate (2-HG) is measured as an indicator of enzyme activity. Ki values are calculated from dose-response curves. STING activation assays may also be performed using reporter cell lines.
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| Cell Assay |
Cellular assays for Alpha-Mangostin involve culturing cancer cell lines or primary cells. Cells are treated with Alpha-Mangostin at varying concentrations (typically 1-50 µM) for 24-72 hours. Cell viability is assessed using MTT or other assays. Apoptosis is measured using annexin V staining or caspase activity assays. STING activation is assessed by measuring IFN-β production.
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| Animal Protocol |
In vivo animal studies for Alpha-Mangostin have been conducted in mouse models of retinal degeneration, liver fibrosis, and other diseases. The compound is typically administered orally or intraperitoneally. Efficacy is assessed by measuring disease-related endpoints such as photoreceptor survival, liver fibrosis markers, or tissue oxidative stress levels. Dosing regimens vary depending on the study.
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| ADME/Pharmacokinetics |
Alpha-Mangostin is soluble in DMSO (82 mg/mL) and ethanol (82 mg/mL) but insoluble in water. For in vivo administration, it can be formulated as a homogeneous suspension in CMC-Na at ≥5 mg/mL or as a clear solution using 5% DMSO, 40% PEG300, 5% Tween 80, and 50% ddH2O. Its molecular weight is 410.46. Detailed PK parameters are limited.
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| Toxicity/Toxicokinetics |
Alpha-Mangostin is generally considered safe at research-relevant doses. It has been used in traditional medicine and is well-tolerated in preclinical studies. However, comprehensive toxicological data are limited. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken.
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| References |
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| Additional Infomation |
α-Catabolin belongs to the xanthones class of compounds with the structure 9H-xanthones, substituted with hydroxyl groups at positions 1, 3, and 6, a methoxy group at position 7, a carbonyl group at position 9, and isopentenyl groups at positions 2 and 8. It is isolated from the stem of Cratoxylum cochinchinense and possesses antioxidant, antibacterial, and antitumor activities. It can be used as an antitumor agent, antibacterial agent, antioxidant, and plant metabolite. It belongs to the xanthones, phenols, and aromatic ethers. Catabolin is a plant/plant extract used in certain over-the-counter (OTC) products. It is not an approved drug. α-Catabolin has been reported in Garcinia cowa, Garcinia merguensis, and several other organisms with relevant data. See also: Mangosteen pericarp (partial).
Alpha-Mangostin is a dietary xanthone with broad biological activities including inhibition of mutant IDH1-R132H (Ki = 2.85 µM) and agonism of human STING. It has anticancer, anti-inflammatory, antioxidant, and neuroprotective properties. The compound is derived from mangosteen and has been used in traditional medicine. It is not approved for clinical use and is available for research purposes. |
| Molecular Formula |
C24H26O6
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|---|---|
| Molecular Weight |
410.4596
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| Exact Mass |
410.172
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| CAS # |
6147-11-1
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| Related CAS # |
beta-Mangostin;20931-37-7
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| PubChem CID |
5281650
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
640.1±55.0 °C at 760 mmHg
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| Melting Point |
182ºC
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| Flash Point |
220.3±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.624
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| LogP |
5.45
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
677
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C2C([H])=C(C(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])=C(C=2C(C2=C1C([H])=C(C(=C2C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])OC([H])([H])[H])O[H])=O)O[H])O[H]
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| InChi Key |
GNRIZKKCNOBBMO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26O6/c1-12(2)6-8-14-16(25)10-19-21(22(14)27)23(28)20-15(9-7-13(3)4)24(29-5)17(26)11-18(20)30-19/h6-7,10-11,25-27H,8-9H2,1-5H3
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| Chemical Name |
1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methylbut-2-enyl)xanthen-9-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~110 mg/mL (~267.99 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4363 mL | 12.1815 mL | 24.3629 mL | |
| 5 mM | 0.4873 mL | 2.4363 mL | 4.8726 mL | |
| 10 mM | 0.2436 mL | 1.2181 mL | 2.4363 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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