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Synonyms | VPS34-IN2 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H17N7 |
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分子量 | 319.36 | CAS No. | 1383716-40-2 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 63 mg/mL (197.26 mM) | ||||||||
Ethanol | 63 mg/mL (197.26 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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in vitro | VPS34 enzymatic function is essential for LC3 lipidation in mammalian cells and PIK-III is a robust inhibitor of autophagy and LC3 lipidation in mammalian cells. In H4 cells, PIK-III inhibits the formation of autolysosomes and increases the cytosolic signal of LC3 under basal conditions and when autophagy is induced with the mTOR inhibitor AZD8055. In a CCCP-induced mitophagy model, PIK-III inhibits the clearance of mitochondria.PIK-III treatment leads to an increase in the levels of LC3-I in H4 and PSN1 cells. In Panc10.05 cells, PIK-III increases the levels of LC3-II in parallel with LC3-I suggesting a cell type-specific response[1]. |
細胞アッセイ | 細胞株 | H4 cells/ HeLa cells |
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濃度 | 2.5μM in H4 cells/5μM in Hela cells | |
反応時間 | overnight for H4 cells/12h for Hela cells | |
実験の流れ | 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. |
, , molecular biosystems, 2017, 13(10):1993-2005
Chronic hypoxia stabilizes 3βHSD1 via autophagy suppression [ Cell Rep, 2024, 43(1):113575] | PubMed: 38181788 |
Targeting autophagy as a therapeutic strategy in pediatric acute lymphoblastic leukemia [ Sci Rep, 2024, 14(1):4000] | PubMed: 38369625 |
Crucial role of iron in epigenetic rewriting during adipocyte differentiation mediated by JMJD1A and TET2 activity [ Nucleic Acids Res, 2023, gkad342] | PubMed: 37158274 |
A mass spectrometric method for in-depth profiling of phosphoinositide regioisomers and their disease-associated regulation [ Nat Commun, 2022, 13(1):83] | PubMed: 35013169 |
Cisplatin resistance can be curtailed by blunting Bnip3-mediated mitochondrial autophagy [ Cell Death Dis, 2022, 13(4):398] | PubMed: 35459212 |
Autophagy Targeting and Hematological Mobilization in FLT3-ITD Acute Myeloid Leukemia Decrease Repopulating Capacity and Relapse by Inducing Apoptosis of Committed Leukemic Cells [ Cancers (Basel), 2022, 14(2)453] | PubMed: 35053612 |
Lysosome docking to WIPI1 rings and ER-connected phagophores occurs during DNAJB12- and GABARAP-dependent selective autophagy of misfolded P23H-rhodopsin [ Mol Biol Cell, 2022, 33(9):ar84] | PubMed: 35704470 |
Protective Mechanism of Berberine on Human Retinal Pigment Epithelial Cells against Apoptosis Induced by Hydrogen Peroxide via the Stimulation of Autophagy [ Oxid Med Cell Longev, 2021, 2021:7654143] | PubMed: 34422209 |
GABARAP sequesters the FLCN-FNIP tumor suppressor complex to couple autophagy with lysosomal biogenesis [ Sci Adv, 2021, 7(40):eabj2485] | PubMed: 34597140 |
Sorting nexin 5 mediates virus-induced autophagy and immunity [ Nature, 2020, 10.1038/s41586-020-03056-z] | PubMed: 33328639 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。