2. NF-κB
  3. Keap1-Nrf2
  4. ML334

ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.

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ML334 Chemical Structure

ML334 Chemical Structure

CAS No. : 1432500-66-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of ML334:

ML334 Related Antibodies

Top Publications Citing Use of Products

    ML334 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals. 2023, 16(1), 14.

    Dehydroeburicoic acid (DEA; 10 µM; 8 h) or ML334 (10 µM; 8 h) inhibit the Keap1-Nrf2 interaction, and there was a 45% reduction of Keap1 co-precipitated with Nrf2 for DEA as compared to 12% inhibition for ML334, in human normal liver cell line LO2 cells.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity[1][2].

    IC50 & Target

    Ki: 1 μM (Keap1)[2]
    In Vitro

    ML334 (LH601A; 50-100 μM; 6-16 hours; HEK293 cells) treatment increases NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. And also enhances HO-1 mRNA expression between 4- and 7-fold at 6 h, with lesser fold-changes at 16 h[1].
    ? ML334 (LH601A; 50-100 μM; 16 hours; HEK293 cells) treatment induces HO-1 and TRX1 proteins in HEK293 cells[1].
    ? ML334 (LH601A) stimulates NRF2 expression and nuclear translocation in HEK293 cells[1].

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

    ML334 Related Antibodies

    RT-PCR[1]

    Cell Line: HEK293 cells
    Concentration: 50 μM or 100 µM
    Incubation Time: 6 hours, 16 hours
    Result: Increased NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. Enhanced HO-1 mRNA expression between 4- and 7-fold at 6 h.

    Western Blot Analysis[1]

    Cell Line: HEK293 cells
    Concentration: 50 μM or 100 µM
    Incubation Time: 16 hours
    Result: Enhanced HO-1 and TRX1 protein expression at 16 h.
    Molecular Weight

    446.50

    Formula

    C26H26N2O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=CC=C1C2=O)N2C[C@@H]3C4=CC=CC=C4CCN3C([C@H]5[C@H](CCCC5)C(O)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 44.65 mg/mL (100.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 44.65 mg/mL (100.00 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2396 mL 11.1982 mL 22.3964 mL
    5 mM 0.4479 mL 2.2396 mL 4.4793 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 (stored under nitrogen). 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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    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: ≥ 5 mg/mL (11.20 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    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: 99.76%

    COA (254 KB) LCMS (87 KB)

    Handling Instructions (2659 KB)
    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 (stored under nitrogen). 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 / Ethanol 1 mM 2.2396 mL 11.1982 mL 22.3964 mL 55.9910 mL
    5 mM 0.4479 mL 2.2396 mL 4.4793 mL 11.1982 mL
    10 mM 0.2240 mL 1.1198 mL 2.2396 mL 5.5991 mL
    15 mM 0.1493 mL 0.7465 mL 1.4931 mL 3.7327 mL
    20 mM 0.1120 mL 0.5599 mL 1.1198 mL 2.7996 mL
    25 mM 0.0896 mL 0.4479 mL 0.8959 mL 2.2396 mL
    30 mM 0.0747 mL 0.3733 mL 0.7465 mL 1.8664 mL
    40 mM 0.0560 mL 0.2800 mL 0.5599 mL 1.3998 mL
    50 mM 0.0448 mL 0.2240 mL 0.4479 mL 1.1198 mL
    60 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9332 mL
    80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.6999 mL
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    ML334 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    ML3341432500-66-7LH601AML 334ML-334Keap1-Nrf2AntioxidantresponseelementsnucleartranslocationNQO1TRX1Inhibitorinhibitorinhibit

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