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  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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MRT67307 hydrochloride 的其他形式现货产品:

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Other Forms of MRT67307 hydrochloride:

    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 抑制 IKKεTBK1,体外浓度为 0.1 mM ATP 时,IC50 值为 160 和 19 nM,但即使浓度为 10 μM[1],也不抑制 IKKα 或 IKKβ >。
    MRT67307 (2 μM) 可防止骨髓来源的巨噬细胞 (BMDM) 中 IRF3 的磷酸化。MRT67307 (2 μM) 不会抑制 poly (I:C)[1]JNKp38 MAPK 的激活。
    MRT67307 (1 nM-10 μM) 可防止 IFNβ 的产生在巨噬细胞中[1]
    MRT67307 (10 μM) 足以将磷酸化 ATG13 降低至控制水平[2]
    MRT67307 (10 μM) 阻断小鼠胚胎成纤维细胞 (MEF) 中的自噬[2]
    MRT67307 (5 μM;4 小时) 消除 293T 细胞中 TBK1/IKKε 诱导的 CYLD 磷酸化[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
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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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