1. NF-κB Autophagy
  2. IKK ULK Autophagy
  3. MRT67307

MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.

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MRT67307 Chemical Structure

MRT67307 Chemical Structure

CAS No. : 1190378-57-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
5 mg USD 96 In-stock
10 mg USD 156 In-stock
50 mg USD 660 In-stock
100 mg USD 852 In-stock
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of MRT67307:

Top Publications Citing Use of Products

    MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Med. 2018 Aug;24(8):1143-1150.  [Abstract]

    Immunoblot of pSTAT1, STAT1 and β-actin levels in H69AR cells±200 ng/mL IFNg 10 min pulse followed by 24 h chase in media with DMSO, Ruxolitinib (100 nM) or MRT67307 (1 µM).

    MRT67307 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2015 Jan 21;6:6074.  [Abstract]

    MRT67307 efficiently inhibits the AKT degradation. IB analysis using WT CD4+ T cells, pretreated for 1 h with a TBK1 inhibitor, MRT67307, of solvent control DMSO and subsequently stimulated for the indicated times with anti-CD3 plus anti-CD28 in the presence of a protein synthesis inhibitor, Cycloheximide.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells[2].

    IC50 & Target[1][2]

    TBK1

    19 nM (IC50, at 0.1 mM ATP)

    IKKε

    160 nM (IC50, at 0.1 mM ATP)

    ULK2

    38 nM (IC50)

    ULK1

    45 nM (IC50)

    Autophagy

     

    In Vitro

    MRT67307 inhibits IKK and TBK1 with IC50 values of 160 and 19 nM when assayed at 0.1 mM ATP in vitro, but did not inhibit IKKα or IKKβ even at 10 μM[1].
    MRT67307 (2 μM) prevents the phosphorylation of IRF3 in bone-marrow-derived macrophages (BMDMs). MRT67307 (2 μM) dose not suppresse the activation of JNK or p38 MAPK by poly(I:C)[1].
    MRT67307 (1 nM-10 μM) prevents the production of IFNβ in macrophages[1].
    MRT67307 (10 μM) is sufficient to reduce phospho-ATG13 to control levels[2].
    MRT67307 (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs)[2].
    MRT67307 (5 μM; 4 h) abrogates TBK1/IKKε-induced CYLD phosphorylation in 293T cells[3].

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

    Western Blot Analysis[3]

    Cell Line: 293T cells
    Concentration: 5 µM
    Incubation Time: 4 hours
    Result: Abrogated TBK1/IKKε-induced CYLD phosphorylation.
    Molecular Weight

    464.60

    Formula

    C26H36N6O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NCCCNC1=NC(NC2=CC=CC(CN3CCOCC3)=C2)=NC=C1C4CC4)C5CCC5

    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 : ≥ 100 mg/mL (215.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1524 mL 10.7619 mL 21.5239 mL
    5 mM 0.4305 mL 2.1524 mL 4.3048 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.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (5.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.38 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.

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

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    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: 99.34%

    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 2.1524 mL 10.7619 mL 21.5239 mL 53.8097 mL
    5 mM 0.4305 mL 2.1524 mL 4.3048 mL 10.7619 mL
    10 mM 0.2152 mL 1.0762 mL 2.1524 mL 5.3810 mL
    15 mM 0.1435 mL 0.7175 mL 1.4349 mL 3.5873 mL
    20 mM 0.1076 mL 0.5381 mL 1.0762 mL 2.6905 mL
    25 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1524 mL
    30 mM 0.0717 mL 0.3587 mL 0.7175 mL 1.7937 mL
    40 mM 0.0538 mL 0.2690 mL 0.5381 mL 1.3452 mL
    50 mM 0.0430 mL 0.2152 mL 0.4305 mL 1.0762 mL
    60 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8968 mL
    80 mM 0.0269 mL 0.1345 mL 0.2690 mL 0.6726 mL
    100 mM 0.0215 mL 0.1076 mL 0.2152 mL 0.5381 mL
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    MRT67307 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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    Cat. No.:
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