1. NF-κB Apoptosis
  2. Keap1-Nrf2 Ferroptosis
  3. ML385

ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.

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

ML385 Chemical Structure

ML385 Chemical Structure

CAS No. : 846557-71-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 68 In-stock
Solution
10 mM * 1 mL in DMSO USD 68 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 90 In-stock
25 mg USD 190 In-stock
50 mg USD 310 In-stock
100 mg USD 490 In-stock
200 mg USD 750 In-stock
500 mg   Get quote  
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Customer Review

Based on 278 publication(s) in Google Scholar

Top Publications Citing Use of Products

266 Publications Citing Use of MCE ML385

RT-PCR
IHC
WB
IF

    ML385 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Feb 24;113:154726.

    ML385 (10 μM; pretreate for 1 h) decreases Dehydroepiandrosterone (DHEA)-induced upregulation of nuclear Nrf2, HO-1 and NQO1 protein levels in both LMH cells and primary chicken hepatocytes.

    ML385 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Apr 7;2019:3501059.  [Abstract]

    Western blot of Nrf2 and HO-1 protein expression levels with the treatment of HEMA, HEMA+BHQ, and HEMA+ML385.

    ML385 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Apr 7;2019:3501059.  [Abstract]

    Immunofluorescence analysis of Nrf2 expression and nuclear translocation. Green fluorescence represents Nrf2, and blue fluorescence represents nucleus of hDPCs. Data represent mean ± standard deviations (n = 3).

    ML385 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Mar 18;2019:2853534.  [Abstract]

    The protein expression levels of Nrf2 (nucleus), Nrf2 (cytoplasm), HO-1, p-NF-κB p65, NF-κB p65, and ICAM-1 proteins are analyzed by Western blot with or without the treatment of H2O2, SAA and ML385.

    ML385 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Oct 24;9(1):4429.   [Abstract]

    QPCR detecting NQO1 and GCLC genes in vector or HPV16 E7-expressing HaCaT cells treated with or without 10 μM ML385 for 24 h.

    ML385 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2018 Oct;175(19):3747-3757.  [Abstract]

    Western blot of whole liver homogenate for p-JNK and 3-NT in mice with or without Chloroquine (CQ; 60 mg/kg) at 6 h.

    ML385 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Sep;155:494-509.  [Abstract]

    THP-1 cells are incubated with Cardamonin (30 μM), ML385 (5 μM) and ML385 + Cardamonin for 21 h, stimulated with LPS (2 μg/mL) for 3 h, and followed by ATP (5 mM) treatment for 30 min. The protein levels of NLRP3, cleaved caspase-1, ASC and cleaved IL-1β are detected by western blotting assay.

    ML385 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Dec 13;9:1444.  [Abstract]

    Seven days after the last MPTP intoxication, nucleus, and cytosol isolated from SNpc and striatum from all groups (sham, KOK, KOK+ML385, ML385, KOK, ML385) are subjected to Western blot assay to quantify changes in Nrf2 nuclear translocation and NQO1 expression, respectively.

    ML385 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Dec 13;9:1444.  [Abstract]

    Seven days after the last MPTP intoxication, SNpc and striatal sections (n = 3 per brain) are subjected to immunofluorescence staining using Nrf2 and NQO1 antibodies with the treatments (sham, KOK, KOK+ML385, ML385, KOK, ML385).

    ML385 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, ML385 alone or combined with lycopene.

    ML385 purchased from MedChemExpress. Usage Cited in: Exp Gerontol. 2017 Dec 15;100:77-86.  [Abstract]

    Cells are treated with ML385 at the concentration of 5 μM for 12 h. The expression of Nrf2 and its translocation into nucleus are determined using western blot analysis.

    ML385 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Dec 26;1864(3):882-890.  [Abstract]

    RAW264.7 cells are transfected with ML385 (5 μM) in the presence of Tan C (10 μM) for 24 h. Prdx1 and Nrf2 protein expression is determined by Western blotting
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.

    IC50 & Target

    IC50: 1.9 μM (NRF2)[1]

    In Vitro

    ML385 interacts with NRF2 and affects the DNA binding activity of the NRF2-MAFG protein complex. The addition of ML385 decreases anisotropy in a dose-dependent manner, with an IC50 of 1.9 μM. A dose-dependent reduction in the NRF2 transcriptional activity is observed and the maximum inhibitory concentration is 5 μM by ML385. Treatment with ML385 leads to a significant reduction in NRF2 and downstream target gene expression selectively in KEAP1 mutant H460 cells. ML385 selectively affects the colony forming ability or growth of lung cancer cells with gain of NRF2 function[1].

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

    In Vivo

    ML385 in combination with carboplatin leads to a significant reduction in tumor cell proliferation, demonstrated by fewer Ki-67 positive cells. Tumor samples treated with ML385 show a significant reduction in NRF2 protein level and its downstream target genes[1].
    ML385 (intraperitoneal injection; 30 mg/kg; 7 days) weakens the therapeutic effects of MSC-Exo on inflammation-induced astrocytic activation in mice, and reduces reactive astrogliosis, NF-κB deactivation[3].

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

    Animal Model: 8-week-old C57B/6 male mice[3]
    Dosage: 30 mg/kg; 7 days
    Administration: Intraperitoneal injection
    Result: Reversed inhibition of MSC-Exo on hippocampal astrocytic activation in vivo.
    Molecular Weight

    511.59

    Formula

    C29H25N3O4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=NC(C2=CC=C(N(C(C3=C(C)C=CC=C3)=O)CC4)C4=C2)=C(C)S1)CC5=CC(OCO6)=C6C=C5

    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 : 25 mg/mL (48.87 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 1.9547 mL 9.7735 mL 19.5469 mL
    5 mM 0.3909 mL 1.9547 mL 3.9094 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
    =
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    ×
    Volume
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    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

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    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: ≥ 2.5 mg/mL (4.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2 mg/mL (3.91 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2 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 (20.0 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.

    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (19.55 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 9.01 mg/mL (17.61 mM); Clear solution; Need ultrasonic

    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: 99.96%

    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 1.9547 mL 9.7735 mL 19.5469 mL 48.8673 mL
    5 mM 0.3909 mL 1.9547 mL 3.9094 mL 9.7735 mL
    10 mM 0.1955 mL 0.9773 mL 1.9547 mL 4.8867 mL
    15 mM 0.1303 mL 0.6516 mL 1.3031 mL 3.2578 mL
    20 mM 0.0977 mL 0.4887 mL 0.9773 mL 2.4434 mL
    25 mM 0.0782 mL 0.3909 mL 0.7819 mL 1.9547 mL
    30 mM 0.0652 mL 0.3258 mL 0.6516 mL 1.6289 mL
    40 mM 0.0489 mL 0.2443 mL 0.4887 mL 1.2217 mL
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    ML385 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.

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    Product Name:
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    Cat. No.:
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