产品说明
一般描述
A cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.
A cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 & mTORC2 (IC50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 µM ATP), with much reduced potency against MKK1 and PI 3-Kα (IC50 ~9 µM) and little or no activity toward more than 200 other protein and lipid kinases, including Akt, ATR, DNA-PK, PDK1, and PI 3-Kβ/γ/δ. Shown to effectively inhibit cellular mTOR phosphorylation on Ser2448/2481 as well as the phosphorylation and activation of mTORC1/2 downstream effector molecules such as Akt, S6K, 4E-BP1, but not RSK or Erk1/2, kinases that are not regulated by mTOR. Although Ku-63794 is shown not to affect IGF-1-induced Akt phosphorylation on Ser308 by PDK1 in mTORC2 knockout MEF cultures, Ku-63794 treatment of mTORC2-expressing MEF cells is shown to inhibit IGF-1-induced Akt Ser308 phosphorylation.
包装
5 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
其他说明
Malagu, K., et al. 2009. Bioorg. Med. Chem. Lett.19, 5950.
Garcia-Martinez, J.M., et al. 2009. Biochem. J.421, 29.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C25H31N5O4 |
分子量 | 465.54 |
MDL编号 | MFCD11977741 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | pale yellow |
溶解性 | DMSO: 15 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich