PIK-III

Catalog No.S7683 Synonyms: VPS34-IN2

PIK-III Chemical Structure

Molecular Weight(MW): 319.36

PIK-III, 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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1 Customer Review

  • LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm

    molecular biosystems, 2017. PIK-III purchased from Selleck.

Purity & Quality Control

Choose Selective Autophagy Inhibitors

Biological Activity

Description PIK-III, 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.
Targets
Vps34 [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
0.018μM 1.2μM
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].

Protocol

Cell Research:

[1]

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  • Cell lines: H4 cells/ HeLa cells
  • Concentrations: 2.5μM in H4 cells/5μM in Hela cells
  • Incubation Time: overnight for H4 cells/12h for Hela cells
  • Method:

    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)

Solubility (25°C)

In vitro DMSO 63 mg/mL (197.26 mM)
Ethanol 63 mg/mL (197.26 mM)
Water 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.

Chemical Information

Molecular Weight 319.36
Formula

C17H17N7

CAS No. 1383716-40-2
Storage powder
in solvent
Synonyms VPS34-IN2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID