1. NF-κB
  2. Keap1-Nrf2

ML385 

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

ML385 is a novel and specific NRF2 inhibitor.

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 87 In-stock
5 mg USD 78 In-stock
10 mg USD 126 In-stock
25 mg USD 264 In-stock
50 mg USD 468 In-stock
100 mg USD 804 In-stock
200 mg USD 1440 In-stock
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 LY294002 5 μM for 2 h followed by treated with MANF 200 ng/mL for another 12 h, and then cell lysates are immunoblotted to assess the phosphorylation of Akt, GSK3β, and Nrf2.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    ML385 is a novel and specific NRF2 inhibitor.

    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].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.9699 mL 9.8493 mL 19.6986 mL
    5 mM 0.3940 mL 1.9699 mL 3.9397 mL
    10 mM 0.1970 mL 0.9849 mL 1.9699 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    ML385 is prepared in Solutol/Cremophor EL/polyethylene glycol 400/water [15/10/35/40,v/v/v/v].

    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

    507.65

    Formula

    C₃₁H₂₉N₃O₂S

    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

    Solvent & Solubility

    DMSO: ≥ 30 mg/mL

    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].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.59%

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