475990

mTOR Inhibitor IV, Ku-63794

The mTOR Inhibitor IV, Ku-63794, also referenced under CAS 938440-64-3, controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 别名: mTOR Inhibitor IV, Ku-63794, rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794
• 经验公式（希尔记法）: C₂₅H₃₁N₅O₄
• CAS号: 938440-64-3
• 分子量: 465.54
• MDL號碼: MFCD11977741
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: pale yellow
• 溶解度: DMSO: 15 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• InChI: 1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+
• InChI 密鑰: RFSMUFRPPYDYRD-CALCHBBNSA-N

说明

一般說明

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.

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

Malagu, K., et al. 2009. Bioorg. Med. Chem. Lett.19, 5950.
Garcia-Martinez, J.M., et al. 2009. Biochem. J.421, 29.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable