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  3. Dimethyl fumarate

Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.

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

Dimethyl fumarate Chemical Structure

Dimethyl fumarate Chemical Structure

CAS No. : 624-49-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
500 mg USD 55 In-stock
5 g USD 73 In-stock
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Based on 28 publication(s) in Google Scholar

Other Forms of Dimethyl fumarate:

Top Publications Citing Use of Products

    Dimethyl fumarate purchased from MedChemExpress. Usage Cited in: Nature. 2023 Mar;615(7952):490-498.  [Abstract]

    Both Fumarate hydratase-IN-1 (FHIN1) and Dimethyl fumarate (DMF) treatment limit IFNβ-induced STAT1 and JAK1 phosphorylation in BMDMs.

    Dimethyl fumarate purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Feb 14;106697.  [Abstract]

    The oligomerized MLKL induced by TSI in both J774A.1 (Fig. E) and BMDMs (Fig. F) are almost completely inhibited by Dimethyl fumarate (DMF; 25, 50 μM; 3 h) treatment in these murine macrophages.

    Dimethyl fumarate purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2018 Aug 16;10(8):2016-2036.  [Abstract]

    Relative changes in the expression of Nrf2, pNrf2 and HO-1 after treatment with D-gal alone or combined with DMF or lycopene.

    Dimethyl fumarate purchased from MedChemExpress. Usage Cited in: J Mol Endocrinol. 2018 Oct 15;61(4):163-172.  [Abstract]

    Keratinocytes are subjected to normal glucose (NG), H2O2, or high glucose (HG) in the presence or absence of DMF, to measure the levels of NRF2 protein.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research[1][2].

    In Vitro

    Dimethyl fumarate (DMF; 20-200 μM; 24 hours) treatment dose-dependently reduces the viability of SGC-7901, HT29, HCT116 and CT26 cancer cells[1].
    Dimethyl fumarate (DMF; 100 μM; 3-24 hours) significantly activates JNK, p38 and ERK in CT26 cells[1].
    Dimethyl fumarate induces necroptosis in colon cancer cells and the mechanism involves GSH depletion, an increase in ROS and activation of MAPKs-mediated signalling[1].
    Dimethyl fumarate inhibits dendritic cell (DC) maturation by reducing inflammatory cytokine production (IL-12 and IL-6) and the expression of MHC class II, CD80, and CD86. Dimethyl fumarate impairs NF-κB signaling via reduced p65 nuclear translocalization and phosphorylation. Dimethyl fumarate inhibits maturation of DCs and subsequently Th1 and Th17 cell differentiation by suppression of both NF-κB and ERK1/2-MSK1 signaling[2].
    Dimethyl fumarate (DMF), an immune modulator and inducer of the antioxidant response, suppresses HIV replication and neurotoxin release[3].

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

    Cell Viability Assay[1]

    Cell Line: SGC-7901, HT29, HCT116 and CT26 cells
    Concentration: 20 μM, 50 μM, 100 μM, 200 μM
    Incubation Time: 24 hours
    Result: Reduced cell viability in SGC-7901, HT29, HCT116 and CT26 cancer cells.

    Western Blot Analysis[1]

    Cell Line: CT26 cancer cells
    Concentration: 100 μM
    Incubation Time: 3 hours, 6 hours, 12 hours, 24 hours
    Result: Significantly activated JNK, p38 and ERK in CT26 cells after treatment from 3 to 24 h.
    In Vivo

    Dimethyl fumarate (DMF; 50 mg/kg; oral gavage; daily; for 7 days) treatment is shown to upregulate the mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes, attenuate 6-OHDA induced striatal oxidative stress and inflammation in C57BL/6 mice[4].

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

    Animal Model: Male C57BL/6 mice (8-week-old)[4]
    Dosage: 50 mg/kg
    Administration: Oral gavage; daily; for 7 days
    Result: Was shown to upregulate mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes.
    Clinical Trial
    Molecular Weight

    144.13

    Formula

    C6H8O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(OC)/C=C/C(OC)=O

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 41.67 mg/mL (289.11 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 6.9382 mL 34.6909 mL 69.3818 mL
    5 mM 1.3876 mL 6.9382 mL 13.8764 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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • 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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    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: ≥ 2.08 mg/mL (14.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (14.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 2 mg/mL (13.88 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    • Protocol 2

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 7.5 mg/mL (52.04 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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: 99.91%

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 6.9382 mL 34.6909 mL 69.3818 mL 173.4545 mL
    5 mM 1.3876 mL 6.9382 mL 13.8764 mL 34.6909 mL
    10 mM 0.6938 mL 3.4691 mL 6.9382 mL 17.3455 mL
    15 mM 0.4625 mL 2.3127 mL 4.6255 mL 11.5636 mL
    20 mM 0.3469 mL 1.7345 mL 3.4691 mL 8.6727 mL
    25 mM 0.2775 mL 1.3876 mL 2.7753 mL 6.9382 mL
    30 mM 0.2313 mL 1.1564 mL 2.3127 mL 5.7818 mL
    40 mM 0.1735 mL 0.8673 mL 1.7345 mL 4.3364 mL
    50 mM 0.1388 mL 0.6938 mL 1.3876 mL 3.4691 mL
    60 mM 0.1156 mL 0.5782 mL 1.1564 mL 2.8909 mL
    80 mM 0.0867 mL 0.4336 mL 0.8673 mL 2.1682 mL
    100 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7345 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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