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KU-0063794

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Chemical Structure| 938440-64-3 同义名 : -
CAS号 : 938440-64-3
货号 : A119369
分子式 : C25H31N5O4
纯度 : 99%+
分子量 : 465.54
MDL号 : MFCD11977741
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(34.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 0.66 mg/mL clear

PO 0.5% CMC-Na 48 mg/mL suspension

生物活性
靶点

  • mTORC1

    mTORC1, IC50:~10 nM

  • mTORC2

    mTORC2, IC50:~10 nM
描述 The mTOR (mammalian target of rapamycin) protein kinase plays a key role in signalling pathways regulating cell growth and proliferation. There are two mTOR complexes characterized, mTORC1 and mTORC2. KU-0063794 is a specific mTORC1 and mTORC2 inhibitor (IC50=∼10 nM, assayed by activity of endogenous immunoprecipitated mTORC on its subtrates). Ku-0063794 can inhibit the downstream of mTORC1, pS6K-T229/389, pS6P-S235, as well as the downstream of mTORC2 pAKT-s473 and its substrates PRAS40 at Thr246, GSK3α/β at Ser21/Ser9 and Foxo-1/3a at Thr24/Thr32, at the concentration 30-1000nM in HEK-293 cell line culture in full media or under IGF1 stimulation. This demonstrates Ku-0063794 can inhibit both mTORC1 and 2 activity in vitro. Ku-0063794 can suppress growth of both wild-type and mLST8-deficient MEFs more markedly than rapamycin and increased the proportion of cells in G1 by 1.5-fold. [1]
作用机制 KU-0063794 is an ATP competitive mTOR inhibitor. [1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
786-O 100-2000 nM Function Assay 10-180 min inhibits both mTORC1 and mTORC2 as indicated by the decrease in phosphorylation of downstream effectors 23349989
786-O 300-4000 nM Cell Viability Assay 24-96 h suppresses the cell viability in both time and dose dependent manner 23349989
786-O 2 µM Function Assay 72 h induces G1 cell cycle arrest and autophagy 23349989
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.48mL

4.30mL

2.15mL