化合物 KU0063794|T2475|TargetMol

KU-0063794
938440-64-3

￥221 1mg 起订

￥493 5mg 起订

￥897 10mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 KU0063794

英文名称：: KU-0063794

CAS号：: 938440-64-3

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.35%

产品类别：: 抑制剂

货号：: T2475

Product Introduction

Bioactivity

名称	KU-0063794
描述	KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
细胞实验	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)
激酶实验	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.
体内活性	KU-0063794但不是雷帕霉素以剂量依赖性方式抑制SGK1活性和Ser422磷酸化以及其生理学底物NDGR1,与S6K1和Akt磷酸化程度相同,而KU-0063794不抑制佛波酯诱导的ERK或RSK磷酸化和RSK激活。与雷帕霉素相比,KU-0063794在Thr37,Thr46和Ser65诱导4E-BP1完全去磷酸化方面表现出更显著的效力。KU-0063794抑制野生型和mLST8-缺陷型MEFs细胞生长,也诱导细胞周期停在G1期,比雷帕霉素效果更明显。与mTOR抑制剂PP242相比,KU-0063794对mTOR表现出更高的特异性,因为对PI3K或其他76种激酶无效。在HEK-293细胞中,30 nM的KU-0063794足以通过阻断疏水基序（Thr389）的磷酸化和随后T环残基（Thr229）的磷酸化来快速消除S6K1活性。100-300 nM的KU-0063794也完全抑制氨基酸诱导的S6K1和S6蛋白的磷酸化。类似于S6K1,KU-0063794以剂量依赖性和时间依赖性方式抑制Ser2448处的mTORC1和Ser2481处的mTORC2的磷酸化。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 4.7 mg/mL (10 mM)
关键字	KU-0063794 \| Inhibitor \| mTOR \| KU0063794 \| Mammalian target of Rapamycin \| KU 0063794 \| inhibit
相关产品	α-Hydroxyglutaric Acid Lithium \| P-2281 \| Capivasertib \| Rapamycin \| Bimiralisib \| L-Leucine \| GDC0084 \| Tacrolimus \| Dihydromyricetin \| PI3K/Akt/mTOR-IN-2 \| Sapanisertib \| (+)-Usnic acid
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 高选择性抑制剂库 \| 临床前化合物库 \| 抗肥胖化合物库 \| 抗氧化化合物库

KU-0063794|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务