化合物 WYE687【1062161-90-3】产品图
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化合物 WYE687【1062161-90-3】

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  • ¥110 - 896
  • TargetMol
  • T6732
  • 2026年07月07日
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    • 文献和实验
    • 技术资料
    • CAS号

      1062161-90-3

    • 规格

      1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg

    规格:1mLx10mM(inDMSO)产品价格:¥236.0
    规格:2mg产品价格:¥110.0
    规格:5mg产品价格:¥182.0
    规格:10mg产品价格:¥282.0
    规格:25mg产品价格:¥561.0
    规格:50mg产品价格:¥896.0

    Product Introduction

    Bioactivity

    名称 WYE-687
    描述 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
    细胞实验 For cell cycle analysis, cells are seeded in 96-well culture plates at 10,000 cells per well for 24 hours, treated with various inhibitors for 24 hours or 48 hours. Following treatment, cells are harvested, washed with PBS and fixed overnight at -20 °C in 70% ethanol. Cells are washed, stained with propidium iodide and analyzed for cell cycle profile (acquired 5000 cells/well) on Guava PCA-96 instrument according to the Guava Cell Cycle Protocol(Only for Reference)
    激酶实验 DELFIA Format of Purified FLAG-TOR: The routine assays with purified FLAG-TOR (FL and 3.5) are performed in 96-well plates as follows. Enzymes are first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 lM microcystin LR, and 100 lg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL test inhibitor or control vehicle dimethyl sulfoxide (DMSO). The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-TOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1-6 hour) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). The DELFIA detection of the phosphorylated (Thr-389) His6-S6K is performed at room temperature using a monoclonal anti-P(T389)- p70S6K antibody (1A5) labeled with Europium-N1- ITC (Eu) (10.4 Eu per antibody). Fortyfive microliters of the terminated kinase reaction mixture are transferred to a MaxiSorp plate containing 55 μL PBS. The His6-S6K is allowed to attach for 2 hour after which the wells are aspirated and washed once with PBS. One hundred microliters of DELFIA buffer with 40 ng/mL Eu-P(T389)-S6K antibody is added. The antibody binding is continued for 1 hour with gentle agitation. The wells are then aspirated and washed four times with PBS containing 0.05% Tween 20 (PBST). One hundred microliters of DELFIA Enhancement solution is added to each well and the plates are read in a PerkinElmer Victor model plate reader. Data obtained are used to calculate enzymatic activity and enzyme inhibition by potential inhibitors.
    体外活性 免疫复合物激酶检测显示,WYE-687对mTORC2特异性底物His6-AKT或mTORC1底物His6-S6K具有剂量依赖性的抑制作用。WYE-687在细胞模型中剂量依赖性地全面抑制mTOR信号传导和AKT功能。WYE-678在MDA361人乳腺癌细胞中,深度抑制帽依赖型及全局蛋白质合成。WYE-687在多种癌细胞系中显示出抗增殖效果,包括G1期细胞周期阻滞和选择性凋亡。WYE-687在U87 mg、MDA361和LNCap细胞中下调血管生成因子VEGF和HIF-1α。[1]
    存储条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
    溶解度 H2O : 60.2 mg/mL (113.88 mM), Sonication is recommended.
    DMSO : 60.2 mg/mL (113.88 mM), Sonication is recommended.
    10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.78 mM), Sonication is recommended.
    关键字 WYE-687 | WYE687 | WYE 687 | Src | PI3Kγ | PI3Kα | PI3K | Phosphoinositide 3-kinase | p38α | p38MAPK | p38 MAPK | mTOR | Mammalian target of Rapamycin | Inhibitor | inhibit
    相关产品 D-Psicose | Musk ketone | Hyaluronic acid | Methyl eugenol | L-Leucine | Undecane | Dihydromyricetin | Myricetin | Fumaric acid | Bisphenol A | Esculin | Stearamide
    相关库 Inhibitor Library | Angiogenesis related Compound Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Hematonosis Compound Library | Membrane Protein-targeted Compound Library | Immunology/Inflammation Compound Library | Pain-Related Compound Library | Tyrosine Kinase Inhibitor Library

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    图标文献和实验
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      网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。

    • 高能化合物 energy rich compound

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    化合物 WYE687【1062161-90-3】
    ¥110 - 896