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  • Compound 401

    • Compound-401; Compound401
    货号: abs812142
    CAS号: 168425-64-7
    分子式: C16H15N3O2
    分子量: 281.31
    产品说明书
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    货号-规格 货期 价格 数量
    abs812142-5mg 1-2周 ¥1031.00
    - +
    abs812142-10mg 1-2周 ¥1516.00
    - +
    大包装询价
    产品描述
    描述

    Compound 401是一种合成的DNA-PK抑制剂 (IC50 = 0.28 μM)。

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    Compound-401; Compound401
    外观
    Beige solid
    可溶性/溶解性
    DMSO : 6 mg/mL (21.33 mM; Need ultrasonic and warming)
    生物活性
    靶点
    DNA-PK
    In vitro(体外研究)
    Compound 401 is a potent inhibitor of DNA-PK (IC50=0.28 μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC50=5.3 μM) but not p110α/p85α PI3K (IC50>100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr389 and Akt Ser473, respectively). By contrast, there is no direct inhibition of Akt Thr308 phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5 μM or 10 μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1-/- fibroblasts is inhibited in the presence of Compound 401, but TSC1+/+ cells are resistant.
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    • 实验方法 实验条件
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