化合物 KU0063794|T2475|TargetMol

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最小起訂量	1removed
發(fā)貨地	上海
更新日期	2026-04-02

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產(chǎn)品詳情

中文名稱:化合物 KU0063794	英文名稱:KU-0063794
CAS:938440-64-3	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 98.21%	產(chǎn)品類別: 抑制劑
貨號(hào): T2475

Product Introduction

Bioactivity

名稱	KU-0063794
描述	KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
細(xì)胞實(shí)驗(yàn)	Cells are treated with KU-0063794 for 24, 48, and 72 hours, and the medium is changed every 24 hours with freshly dissolved KU-0063794. For the measurement of cell growth, cells are washed once with PBS, and fixed in 4% (v/v) paraformaldehyde in PBS for 15 minutes. After washing once with water, the cells are stained with 0.1% Crystal Violet in 10% ethanol for 20 minutes and washed three times with water. Crystal Violet is extracted from cells with 0.5 mL of 10% (v/v) ethanoic (acetic) acid for 20 minutes. The eluate is then diluted 1:10 in water and absorbance at 590 nm is quantified. For the assessment of cell cycle distribution, cells are harvested by trypsinization, washed once in PBS, and re-suspended in ice-cold aq. 70% (v/v) ethanol. Cells are washed twice in PBS plus 1% (w/v) BSA and stained for 20 minutes in PBS plus 0.1% (v/v) Triton X-100 containing 50 g/mL propidium iodide and 50 g/mL RNase A. The DNA content of cells is determined using a FACSCalibur flow cytometer and CellQuest software. Red fluorescence (585 nm) is acquired on a linear scale, and pulse width analysis is used to exclude doublets. Cell-cycle distribution is determined using FlowJo software.(Only for Reference)
激酶實(shí)驗(yàn)	mTOR complexes kinase assays: HEK-293 cells are freshly lysed in Hepes lysis buffer. Lysate (1-4 mg) is pre-cleared by incubating with 5-20 μL of Protein G-Sepharose conjugated to pre-immune IgG. The lysate extracts are then incubated with 5-20 μL of Protein G-Sepharose conjugated to 5-20 μg of either anti-Rictor or anti-Raptor antibody, or pre-immune IgG. All antibodies are covalently conjugated to Protein G-Sepharose. Immunoprecipitations are carried out for 1 hour at 4 °C on a vibrating platform. The immunoprecipitates are washed four times with Hepes lysis buffer, followed by two washes with Hepes kinase buffer. For Raptor immunoprecipitates used for phosphorylating S6K1, for the initial two wash steps the buffer includes 0.5 M NaCl to ensure optimal kinase activity. GST-Akt1 is isolated from serum-deprived HEK-293 cells incubated with PI-103 (1 μM for 1 hour). GST-S6K1 is purified from serum-deprived HEK-293 cells incubated with rapamycin (0.1 μM for 1 hour). mTOR reactions are initiated by adding 0.1 mM ATP and 10 mM MgCl2 in the presence of various concentrations of KU-0063794 and GST-Akt1 (0.5 μg) or GST-S6K1 (0.5 μg). Reaction are carried out for 30 minutes at 30 °C on a vibrating platform and stopped by addition of SDS sample buffer. Reaction mixtures are then filtered through a 0.22-μm-poresize Spin-X filter and samples are subjected to electrophoresis and immunoblot analysis with the indicated antibodies.
體內(nèi)活性	KU-0063794但不是雷帕霉素以劑量依賴性方式抑制SGK1活性和Ser422磷酸化以及其生理學(xué)底物NDGR1,與S6K1和Akt磷酸化程度相同,而KU-0063794不抑制佛波酯誘導(dǎo)的ERK或RSK磷酸化和RSK激活。與雷帕霉素相比,KU-0063794在Thr37,Thr46和Ser65誘導(dǎo)4E-BP1完全去磷酸化方面表現(xiàn)出更顯著的效力。KU-0063794抑制野生型和mLST8-缺陷型MEFs細(xì)胞生長,也誘導(dǎo)細(xì)胞周期停在G1期,比雷帕霉素效果更明顯。與mTOR抑制劑PP242相比,KU-0063794對(duì)mTOR表現(xiàn)出更高的特異性,因?yàn)閷?duì)PI3K或其他76種激酶無效。在HEK-293細(xì)胞中,30 nM的KU-0063794足以通過阻斷疏水基序（Thr389）的磷酸化和隨后T環(huán)殘基（Thr229）的磷酸化來快速消除S6K1活性。100-300 nM的KU-0063794也完全抑制氨基酸誘導(dǎo)的S6K1和S6蛋白的磷酸化。類似于S6K1,KU-0063794以劑量依賴性和時(shí)間依賴性方式抑制Ser2448處的mTORC1和Ser2481處的mTORC2的磷酸化。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.15 mM), Sonication is recommended. DMSO : 8.06 mg/mL (17.31 mM), Sonication is recommended.
關(guān)鍵字	mTORC2 \| mTORC1 \| mTOR \| Mammalian target of Rapamycin \| KU-0063794 \| KU0063794 \| KU 0063794 \| Inhibitor \| inhibit
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相關(guān)庫	抑制劑庫 \| 抗乳腺癌化合物庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 已知活性化合物庫 \| 氧化還原化合物庫 \| 激酶抑制劑庫 \| 高選擇性抑制劑庫 \| 抗衰老化合物庫 \| 血液病分子庫 \| 免疫/炎癥分子化合物庫 \| 細(xì)胞重編程化合物庫

關(guān)鍵字： KU-0063794|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （14年）	注冊(cè)資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：14年
注冊(cè)資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號(hào)8樓

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