1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  2. Reactive Oxygen Species (ROS) Ferroptosis Malate Dehydrogenase (MDH)
  3. MDH1-IN-2

MDH1-IN-2 (Compound 7c) is a selective MDH1 inhibitor, with IC50 values of 2.27 and 27.47 μM for MDH1 and MDH2, respectively. MDH1-IN-2 can reduce the generation of ROS by inhibiting the conversion of 2-Ketoglutaric acid (HY-W013636) to α-Hydroxyglutaric acid (HY-113038B) mediated by MDH1, thereby suppressing 2-Ketoglutaric acid (HY-W013636)-induced ferroptosis.

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

CAS No. : 2143463-35-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MDH1-IN-2

Flow Cytometry
Bio/Physico-chemical Assay

    MDH1-IN-2 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2023 Jun 12;9(1):182.  [Abstract]

    OCI-LY1 and OCI-LY10 cells were treated with 10 μM MDH1-IN-2 pre-treatment followed by 15 mM DM-αKG. DCFDA assay was applied to detect intracellular ROS levels, represented by flow cytometry plots.

    MDH1-IN-2 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2023 Jun 12;9(1):182.  [Abstract]

    OCI-LY1 and OCI-LY10 cells were treated with 10 μM MDH1-IN-2 pre-treatment followed by 15 mM DM-αKG. Supernatant 2-HG levels of drug-treated cells were detected by 2-HG assay.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MDH1-IN-2 (Compound 7c) is a selective MDH1 inhibitor, with IC50 values of 2.27 and 27.47 μM for MDH1 and MDH2, respectively. MDH1-IN-2 can reduce the generation of ROS by inhibiting the conversion of 2-Ketoglutaric acid (HY-W013636) to α-Hydroxyglutaric acid (HY-113038B) mediated by MDH1, thereby suppressing 2-Ketoglutaric acid (HY-W013636)-induced ferroptosis[1][2].

    In Vitro

    MDH1-IN-2 (10 μM; pre-treatment) reduces intracellular ROS production and α-Hydroxyglutaric acid (HY-113038B) production in the supernatant induced by Dimethyl 2-oxoglutarate (HY-44134) in OCI-LY1 and OCI-LY10 cells[2].

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

    Molecular Weight

    427.53

    Formula

    C25H33NO5

    CAS No.
    Appearance

    Solid

    Color

    White to light brown

    SMILES

    O=C(OC)C1=CC=C(OC)C(NC(COC2=CC=C(C(C)(C)CC(C)(C)C)C=C2)=O)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (58.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3390 mL 11.6951 mL 23.3902 mL
    5 mM 0.4678 mL 2.3390 mL 4.6780 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1 mg/mL (2.34 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1 mg/mL (2.34 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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: 98.70%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3390 mL 11.6951 mL 23.3902 mL 58.4754 mL
    5 mM 0.4678 mL 2.3390 mL 4.6780 mL 11.6951 mL
    10 mM 0.2339 mL 1.1695 mL 2.3390 mL 5.8475 mL
    15 mM 0.1559 mL 0.7797 mL 1.5593 mL 3.8984 mL
    20 mM 0.1170 mL 0.5848 mL 1.1695 mL 2.9238 mL
    25 mM 0.0936 mL 0.4678 mL 0.9356 mL 2.3390 mL
    30 mM 0.0780 mL 0.3898 mL 0.7797 mL 1.9492 mL
    40 mM 0.0585 mL 0.2924 mL 0.5848 mL 1.4619 mL
    50 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1695 mL
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    • Do most proteins show cross-species activity?

      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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    Product Name:
    MDH1-IN-2
    Cat. No.:
    HY-147791
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