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

MRT67307 

Cat. No.: HY-13018 Purity: 99.34%
Handling Instructions

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

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10 mM * 1  mL in DMSO USD 106 In-stock
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10 mg USD 156 In-stock
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50 mg USD 660 In-stock
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100 mg USD 852 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of MRT67307:

Top Publications Citing Use of Products

    MRT67307 purchased from MCE. Usage Cited in: Nat Commun. 2015 Jan 21;6:6074.

    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.

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

    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).

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    • 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 IKKϵ 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].

    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.

    1190378-57-4

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (215.24 mM)

    *"≥" 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
    10 mM 0.2152 mL 1.0762 mL 2.1524 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.34%

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    Keywords:

    MRT67307MRT 67307MRT-67307IKKULKAutophagyIκB kinaseI kappa B kinase Unc-51 like kinaseIKKεTBK-1ULK1ULK2autophagysignaltransductioncancerInhibitorinhibitorinhibit

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    Product name:
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    Cat. No.:
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