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  • 化合物 PIK-III|T6945|TargetMol

化合物 PIK-III|T6945|TargetMol

Vps34-PIK-III
1383716-40-2
395 1mg 起订
568 2mg 起订
997 5mg 起订
上海 更新日期:2024-09-30

TargetMol中国(陶术生物)

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联系人:邵小姐
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邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 PIK-III
英文名称:
Vps34-PIK-III
CAS号:
1383716-40-2
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:
98.43%
产品类别:
抑制剂
货号:
T6945

Product Introduction

Bioactivity

名称Vps34-PIK-III
描述Vps34-PIK-III (VPS34-IN2), a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.
细胞实验To determine whether inhibition of VPS34 function impacts autophagy,LC3 and known autophagy substrates such as damaged mitochondria or the autophagy cargo receptor p62 are monitored. H4 cells expressing mCherry–GFP–LC3 are treated overnight with the indicated compounds, fixed, stained with Hoechst 33342 and imaged by automated acquisition. HeLa cells expressing GFP–Parkin are treated with PIK-III for 12 h followed by the addition of CCCP for 12 h, fixed, stained for endogenous Tom20 and imaged. (Only for Reference)
激酶实验In vitro tyrosine kinase assays.: Assay of IGF-1R-catalyzed substrate phosphorylation of pTG, using a 96-well plate tyrosine kinase assay kit, is performed. We use recombinant epidermal growth factor receptor, immunoprecipitated IR from HEPG2, immunoprecipitated IGF-1R from P6 cells, and IGF-1R immunodepleted supernatant from P6 (representing "non-IGF-1R tyrosine kinases"). After 30-min treatment of the receptors with the desired compounds in the kinase buffer [50 mM HEPES buffer (pH 7.4), 20 mM MgCl2, 0.1 MnCl2, and 0.2 Na3VO4], the kinase reaction is activated by addition of ATP. The phosphorylated polymer substrate is probed with a phosphotyrosine-specific monoclonal antibody conjugated to horseradish peroxidase, clone PT-66. Color is developed with horseradish peroxidase chromogenic substrate O-phenylenediamine dihydrochloride and quantitated by spectrophotometry (ELISA reader). IGF-1R tyrosine autophosphorylation is analyzed by a sandwich ELISA assay. Briefly, 96-well plates are coated overnight at 4°C with 1 μg/well of an antibody to IGF-1R β-subunit. The plates are blocked with 1% BSA in PBS Tween for 1 h, and then 80 μg/well of total protein lysate from the P6 cell line is added. As a negative control we use total protein lysate from the R- cell line. The investigated compounds are added in tyrosine kinase buffer without ATP at room temperature for 30 min before kinase activation with ATP. Kinase assay is performed using the Sigma kit (see above). After spectrophotometry the IC50 values of inhibitors are determined using the REGRESSION function of Statistica program.
体外活性VPS34的酶功能对哺乳动物细胞中的LC3脂质化是必要的,而PIK-III是一种强效的自噬和LC3脂质化抑制剂。在H4细胞中,PIK-III抑制自溶体的形成,并且在基础条件下以及使用mTOR抑制剂AZD8055诱导自噬时增加LC3的胞质信号。在CCCP诱导的线粒体自噬模型中,PIK-III抑制了线粒体的清除。PIK-III处理导致H4和PSN1细胞中LC3-I水平的增加。在Panc10.05细胞中,PIK-III同时增加LC3-II和LC3-I的水平,暗示了一种细胞类型特异性反应[1]。
体内活性DFX诱导的NCOA4依赖的FTH1和FTL的周转在加入PIK-III后被阻断,这表明是一个自噬依赖的过程[2]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (187.88 mM)
Ethanol : 59 mg/mL (184.7 mM)
关键字PI3K | Autophagy | Vps34 PIK III | Vps-34-PIK-III | Vps34-PIK-III | Inhibitor | Phosphoinositide 3-kinase | Vps34PIKIII | inhibit
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PIK-III|||VPS34-IN2|TargetMol

公司简介

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

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