KU-0063794
产品说明书
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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： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 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 |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 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 | |||||
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| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 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 | |
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1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.21mL |
10.74mL 2.15mL 1.07mL |
21.48mL 4.30mL 2.15mL |
