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

MRT67307 hydrochloride 是 IKKεTBK-1 的双抑制剂,IC50 分别为 160 和 19 nM。MRT67307 hydrochloride 也可抑制 ULK1ULK2IC50 分别为 45 和 38 nM。MRT67307 hydrochloride 还抑制细胞自噬 (autophagy)。

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MRT67307 hydrochloride Chemical Structure

MRT67307 hydrochloride Chemical Structure

CAS No. : 2095432-39-4

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Top Publications Citing Use of Products

    MRT67307 hydrochloride purchased from MCE. 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 hydrochloride purchased from MCE. 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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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

     

    体外研究
    (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].

    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.
    分子量

    501.06

    Formula

    C26H37ClN6O2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献

    MRT67307 hydrochloride 相关分类

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    • 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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