化合物 WYE687|T6732|TargetMol

WYE-687
1062161-90-3

￥136 1mg 起订

￥197 2mg 起订

￥346 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 化合物 WYE687

英文名称：: WYE-687

CAS号：: 1062161-90-3

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：: 98.98%

产品类别：: 抑制剂

货号：: T6732

Product Introduction

Bioactivity

Name	WYE-687
Description	WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
Cell Research	For cell cycle analysis, cells are seeded in 96-well culture plates at 10,000 cells per well for 24 hours, treated with various inhibitors for 24 hours or 48 hours. Following treatment, cells are harvested, washed with PBS and fixed overnight at -20 °C in 70% ethanol. Cells are washed, stained with propidium iodide and analyzed for cell cycle profile (acquired 5000 cells/well) on Guava PCA-96 instrument according to the Guava Cell Cycle Protocol(Only for Reference)
Kinase Assay	DELFIA Format of Purified FLAG-TOR: The routine assays with purified FLAG-TOR (FL and 3.5) are performed in 96-well plates as follows. Enzymes are first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 lM microcystin LR, and 100 lg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL test inhibitor or control vehicle dimethyl sulfoxide (DMSO). The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-TOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1-6 hour) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). The DELFIA detection of the phosphorylated (Thr-389) His6-S6K is performed at room temperature using a monoclonal anti-P(T389)- p70S6K antibody (1A5) labeled with Europium-N1- ITC (Eu) (10.4 Eu per antibody). Fortyfive microliters of the terminated kinase reaction mixture are transferred to a MaxiSorp plate containing 55 μL PBS. The His6-S6K is allowed to attach for 2 hour after which the wells are aspirated and washed once with PBS. One hundred microliters of DELFIA buffer with 40 ng/mL Eu-P(T389)-S6K antibody is added. The antibody binding is continued for 1 hour with gentle agitation. The wells are then aspirated and washed four times with PBS containing 0.05% Tween 20 (PBST). One hundred microliters of DELFIA Enhancement solution is added to each well and the plates are read in a PerkinElmer Victor model plate reader. Data obtained are used to calculate enzymatic activity and enzyme inhibition by potential inhibitors.
In vitro	免疫复合物激酶检测显示，WYE-687对mTORC2特异性底物His6-AKT或mTORC1底物His6-S6K具有剂量依赖性的抑制作用。WYE-687在细胞模型中剂量依赖性地全面抑制mTOR信号传导和AKT功能。WYE-678在MDA361人乳腺癌细胞中，深度抑制帽依赖型及全局蛋白质合成。WYE-687在多种癌细胞系中显示出抗增殖效果，包括G1期细胞周期阻滞和选择性凋亡。WYE-687在U87 mg、MDA361和LNCap细胞中下调血管生成因子VEGF和HIF-1α。[1]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : 60.2 mg/mL (100 mM) DMSO : 60.2 mg/mL (100 mM)
Keywords	mTOR \| Mammalian target of Rapamycin \| Phosphoinositide 3-kinase \| WYE 687 \| PI3K \| WYE687 \| inhibit \| WYE-687 \| Inhibitor
Inhibitors Related	(-)-Bornyl acetate \| Quercetin \| Rapamycin \| Quercetin Dihydrate \| Apilimod \| SB 202190 \| L-Leucine \| Nintedanib \| Myricetin \| Isoprenaline hydrochloride \| Erucic acid \| Bakuchiol
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| Anti-Ovarian Cancer Compound Library \| Anti-Obesity Compound Library \| Antioxidant Compound Library \| Pain-Related Compound Library \| Tyrosine Kinase Inhibitor Library

N-[4-[4-(4-吗啉基)-1-[1-(3-吡啶甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶-6-基]苯基]氨基甲酸甲酯|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。

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