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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期:1-2天
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MedChemExpress LLC
- CAS号:
1383716-40-2
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10 mM * 1 mL/1 mg/2 mg/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1230.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥494.0 |
| 规格: | 2 mg | 产品价格: | ¥700.0 |
| 规格: | 5 mg | 产品价格: | ¥1150.0 |
| 规格: | 10 mg | 产品价格: | ¥1850.0 |
| 规格: | 25 mg | 产品价格: | ¥3880.0 |
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Vps34-PIK-III
CAS No. : 1383716-40-2
MCE 国际站:Vps34-PIK-III
产品活性:Vps34-PIK-III是有效选择性的 VPS34 抑制剂,IC50 值为18 nM。
研究领域:PI3K/Akt/mTOR | Autophagy
In Vitro: PIK-III is a selective inhibitor of VPS34 that binds a unique hydrophobic pocket not present in related kinases such as PI3Kα. PIK-III is at least 100-fold-selective for VPS34 over related lipid kinases such as PI3K and the protein kinase mTOR. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, and leads to the stabilization of autophagy substrates. In H4 cells expressing the mCherry-GFP-LC3 reporter PIK-III inhibits the formation of mCherry-positive autolysosomes and increases the cytosolic signal of LC3 under basal conditions and when autophagy is induced with the mTOR inhibitor AZD8055. PIK-III prevents the turnover of GFP-tagged p62 under basal conditions and when autophagy is activated. PIK-III treatment leads to an increase in the levels of LC3-I in H4 and PSN1 cells.
In Vivo: The DFX-induced NCOA4-dependent turnover of FTH1 and FTL is blocked with PIK-III suggesting an autophagy-dependent process.
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文献和实验蛋白激酶,能接受多种上游信号,如 Class I PI3K、IGF-1/2、MAPK,能感受营养和能量的变化。mTOR 存在两种不同形式:对雷帕霉素敏感的 mTOR 复合物1(mTOR1)和对雷帕霉素不敏感的 mTOR 复合物2(mTOR2)。 2)Beclin-1 信号通路:Beclin-1 是酵母自噬基因 Atg6/Vps30 的同源基因,能与多种蛋白结合,如 Vps34(Class III PI3K 的催化亚单位),mTOR,BCL-2 和 BCLXL 蛋白等,beclin-1 是一个
重磅综述:年发文量近 10000,自噬领域第 4 版研究指南发布
and Atg1/ULK1 等蛋白或者基因的检测;⑤对 PtdIns3K (PIK3C3/VPS34) 活性的评估;⑥通过对不同选择性自噬的阐述,以进行特异性自噬检测:比如,线粒体自噬(mitophagy)、聚集体自噬(aggrephagy)、核糖体自噬(ribophagy)、内质网自噬(reticulophagy)、细胞核自噬(nucleophagy)、异源吞噬(xenophagy)、溶酶体自噬 (lysophagy)、脂滴自噬 (lipophagy)、铁自噬 (ferritinophagy) 等;⑦
Measurement of Phosphoinositide 3-Kinase Activity
only PtdIns as a substrate (e.g., mammalian PtdIns 3-kinase and yeast Vps34p) ( 1 ). Generally, PI 3 kinases are now regarded as an important intracellular signal upstream of a variety of biochemical (e.g., activation of Akt/protein kinase B and/or p70
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