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alpha-Mangostin  (Synonyms: α-Mangostin)

Cat. No.: HY-N0328 Purity: 99.64%
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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.

For research use only. We do not sell to patients.

alpha-Mangostin Chemical Structure

alpha-Mangostin Chemical Structure

CAS No. : 6147-11-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 55 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of alpha-Mangostin:

Top Publications Citing Use of Products

    alpha-Mangostin purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Jan;24(1):760-771.  [Abstract]

    MA (alpha-Mangostin) impedes proliferation and induces cell cycle arrest in gallbladder cancer cells. GBC-SD cells are treated with MA, and proliferation was assessed by the EdU assay.

    alpha-Mangostin purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Jan;24(1):760-771.  [Abstract]

    MA (alpha-Mangostin) impedes proliferation and induces cell cycle arrest in gallbladder cancer cells. NOZ cells are treated with MA, and proliferation was assessed by the EdU assay.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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 & Target

    IC50: 2.85 μM (IDH1-R132H)[1]

    Cellular Effect
    Cell Line Type Value Description References
    A-375 IC50
    2.7 μM
    Compound: SST0673
    Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by trypan blue or crystal violet staining based assay
    Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by trypan blue or crystal violet staining based assay
    [PMID: 32435392]
    A-431 IC50
    7.2 μM
    Compound: NSC27593
    Antiproliferative activity against human A-431 cells overexpressing EGFR assessed as cell growth inhibition by MTT assay
    Antiproliferative activity against human A-431 cells overexpressing EGFR assessed as cell growth inhibition by MTT assay
    [PMID: 34995690]
    ASPC1 IC50
    4.02 μM
    Compound: 1
    Cytotoxicity against human AsPC1 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    Cytotoxicity against human AsPC1 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    [PMID: 24717154]
    B16-F10 IC50
    3.23 μM
    Compound: 1
    Cytotoxicity against mouse B16F10 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    Cytotoxicity against mouse B16F10 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    [PMID: 24717154]
    Daoy IC50
    1.9 μM
    Compound: SST0673
    Antiproliferative activity against human DaOY cells assessed as reduction in cell viability incubated for 72 hrs by trypan blue or crystal violet staining based assay
    Antiproliferative activity against human DaOY cells assessed as reduction in cell viability incubated for 72 hrs by trypan blue or crystal violet staining based assay
    [PMID: 32435392]
    DLD-1 IC50
    7.5 μM
    Compound: alpha-mangostin
    Cytotoxicity against human DLD1 cells after 24 hrs by Trypan blue exclusion test
    Cytotoxicity against human DLD1 cells after 24 hrs by Trypan blue exclusion test
    [PMID: 17553685]
    HeLa IC50
    > 10 μM
    Compound: 3
    Inhibition of NFkappa p65 in nuclear extract of human HeLa cells assessed as blockade of NFkappa p65 binding to biotinylated-consesus sequence by ELISA
    Inhibition of NFkappa p65 in nuclear extract of human HeLa cells assessed as blockade of NFkappa p65 binding to biotinylated-consesus sequence by ELISA
    [PMID: 21428375]
    HeLa IC50
    11.95 μM
    Compound: NSC27593
    Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by MTT assay
    Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by MTT assay
    [PMID: 34995690]
    HeLa S3 IC50
    > 10 μM
    Compound: 12
    Cytotoxicity in human HeLaS3 cells incubated for 72 hrs by MTT assay
    Cytotoxicity in human HeLaS3 cells incubated for 72 hrs by MTT assay
    [PMID: 30978023]
    HepG2 IC50
    > 10 μM
    Compound: 12
    Cytotoxicity in human HepG2 cells incubated for 72 hrs by MTT assay
    Cytotoxicity in human HepG2 cells incubated for 72 hrs by MTT assay
    [PMID: 30978023]
    HepG2 IC50
    8.55 μM
    Compound: alpha-Mangostin
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 31343173]
    HL-60 IC50
    6.8 μM
    Compound: 1
    Cytotoxicity against human HL60 cells assessed as cell viability after 72 hrs by Trypan blue exclusion test
    Cytotoxicity against human HL60 cells assessed as cell viability after 72 hrs by Trypan blue exclusion test
    [PMID: 12932141]
    HT-29 IC50
    > 10 μM
    Compound: 12
    Cytotoxicity in human HT-29 cells incubated for 72 hrs by MTT assay
    Cytotoxicity in human HT-29 cells incubated for 72 hrs by MTT assay
    [PMID: 30978023]
    HT-29 IC50
    0.2 μM
    Compound: 3
    Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay
    Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay
    [PMID: 21428375]
    HT-29 ED50
    4.1 μM
    Compound: 3
    Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
    [PMID: 21428375]
    KB IC50
    > 10 μM
    Compound: 12
    Cytotoxicity in human KB cells incubated for 72 hrs by MTT assay
    Cytotoxicity in human KB cells incubated for 72 hrs by MTT assay
    [PMID: 30978023]
    KB IC50
    14.14 μM
    Compound: alpha-mangostin
    Cytotoxicity against human KB cells after 48 hrs by MTT assay
    Cytotoxicity against human KB cells after 48 hrs by MTT assay
    [PMID: 30684866]
    MCF7 IC50
    > 10 μM
    Compound: 12
    Cytotoxicity in human MCF7 cells incubated for 72 hrs by MTT assay
    Cytotoxicity in human MCF7 cells incubated for 72 hrs by MTT assay
    [PMID: 30978023]
    MCF7 IC50
    3.5 μg/mL
    Compound: 6
    Cytotoxicity against human MCF7 cells assessed as [3H]hypoxanthin incorporation after 24 to 72 hrs
    Cytotoxicity against human MCF7 cells assessed as [3H]hypoxanthin incorporation after 24 to 72 hrs
    [PMID: 19296616]
    MCF7 IC50
    9.95 μM
    Compound: alpha-Mangostin
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 31343173]
    MDA-MB-231 IC50
    12.75 μM
    Compound: 105
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33619958]
    MDA-MB-231 IC50
    3.04 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    [PMID: 24717154]
    MRC5 CC50
    7.5 μM
    Compound: alpha-mangostin
    Cytotoxicity against human MRC5 SV2 cells measured after 72 hrs by resazurin based fluorescence assay
    Cytotoxicity against human MRC5 SV2 cells measured after 72 hrs by resazurin based fluorescence assay
    [PMID: 27517813]
    NCI-H460 IC50
    3.23 μM
    Compound: 1
    Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    [PMID: 24717154]
    SW-620 IC50
    2.97 μM
    Compound: 1
    Cytotoxicity against human SW620 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    Cytotoxicity against human SW620 cells assessed as inhibition of cell proliferation after 48 hrs by XTT assay
    [PMID: 24717154]
    In Vitro

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    410.46

    Formula

    C24H26O6

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C2=C(OC3=C1C(C/C=C(C)\C)=C(OC)C(O)=C3)C=C(O)C(C/C=C(C)\C)=C2O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 110 mg/mL (267.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.75 mg/mL (6.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.64%

    References
    Cell Assay
    [1]

    IDH1+/+ and IDH1 MCF10A cells are grown in DMEM/F-12 media, supplemented with 5% horse serum, 20 ng/mL EGF, 0.5 μg/mL hydrocortisone, 10 μg/mL insulin. IDH1+/+ and IDH1 MCF10A cells are seeded in 6 well plates. After an exposure to 5 μM alpha-mangostin. cells are collected after indicated times and the viable cell number is calculated, using hemacytometer counting[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Rats: Male Wistar rats are divided into 3 groups and treated with intraperitoneal injections of TAA (200 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 per weekfor a total of4 weeks. The incidence offibrotic nodules on the liver and the serum levels of the liver enzymes 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.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4363 mL 12.1815 mL 24.3629 mL 60.9073 mL
    5 mM 0.4873 mL 2.4363 mL 4.8726 mL 12.1815 mL
    10 mM 0.2436 mL 1.2181 mL 2.4363 mL 6.0907 mL
    15 mM 0.1624 mL 0.8121 mL 1.6242 mL 4.0605 mL
    20 mM 0.1218 mL 0.6091 mL 1.2181 mL 3.0454 mL
    25 mM 0.0975 mL 0.4873 mL 0.9745 mL 2.4363 mL
    30 mM 0.0812 mL 0.4060 mL 0.8121 mL 2.0302 mL
    40 mM 0.0609 mL 0.3045 mL 0.6091 mL 1.5227 mL
    50 mM 0.0487 mL 0.2436 mL 0.4873 mL 1.2181 mL
    60 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0151 mL
    80 mM 0.0305 mL 0.1523 mL 0.3045 mL 0.7613 mL
    100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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