[CAS NO. 1383716-40-2] PIK-III
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PRODUCTS SPECIFICATIONS [1383716-40-2]
Store
Catalog
SLK-S7683
Brand
Selleck
CAS
1383716-40-2
DESCRIPTION [1383716-40-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 319.36 |
| Molecular Formula | C17H17N7 |
| SMILES | NC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1313 mL | 15.6563 mL | 31.3126 mL |
| 5 mM | 0.6263 mL | 3.1313 mL | 6.2625 mL |
| 10 mM | 0.3131 mL | 1.5656 mL | 3.1313 mL |
| 50 mM | 0.0626 mL | 0.3131 mL | 0.6263 mL |
Description
PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
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.
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