1. NF-κB
  2. Keap1-Nrf2

ML385 

Cat. No.: HY-100523 Purity: 99.59%
Handling Instructions

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 68 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
25 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 310 In-stock
Estimated Time of Arrival: December 31
100 mg USD 490 In-stock
Estimated Time of Arrival: December 31
200 mg USD 750 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

    ML385 purchased from MCE. Usage Cited in: Exp Gerontol. 2017 Oct 25;100:77-86.

    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 MCE. Usage Cited in: Biochim Biophys Acta. 2017 Dec 26;1864(3):882-890.

    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

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

    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 MCE. Usage Cited in: Biochem Pharmacol. 2018 Jul 31;155:494-509.

    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 MCE. Usage Cited in: Aging (Albany NY). 2018 Aug 16;10(8):2016-2036.

    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 MCE. Usage Cited in: Nat Commun. 2018 Oct 24;9(1):4429. 

    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 MCE. Usage Cited in: Front Pharmacol. 2018 Dec.

    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 MCE. Usage Cited in: Front Pharmacol. 2018 Dec.

    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).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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].

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (58.64 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1955 mL 0.9773 mL 1.9547 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      ML385 is dissolved in 100% DMSO to prepare a stock solution, and then diluted it into 5% DMSO solution with PBS before being used[2].

    References
    Cell Assay
    [1]

    cells are treated with ML385 for 36 h. An equal amount of CellTiter-Blue reagent is added to the wells and the fluorescence is measured after 30 min. The CellTiter-Blue reagent is discarded and the Caspase-Glo (100 μL) reagent is added to the cells and incubated at 37°C for an additional 60-90 min. The resulting luminescence is recorded and the caspase activity is normalized to cell number[1].

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

    Animal Administration
    [1]

    Mice: Mice tumor xenografts are randomly allocated into 4 groups: vehicle, ML385, carboplatin, and ML385 in combination with carboplatin. Vehicle, carboplatin (5 mg/kg daily Monday to Friday)18, ML385 (30 mg/kg daily Monday to Friday), or ML385 in combination with carboplatin are administered intraperitoneally for 3 weeks. At the end of treatment period, mice are sacrificed and the tumor, blood, lung, and liver samples are collected[1].

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

    References
    Molecular Weight

    511.59

    Formula

    C₂₉H₂₅N₃O₄S

    CAS No.

    846557-71-9

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.59%

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    Inquiry Information

    Product Name:
    ML385
    Cat. No.:
    HY-100523
    Quantity:

    ML385

    Cat. No.: HY-100523