Home Autophagy Autophagy inhibitor - PI3K inhibitor - LC3 inhibitor PIK-III For research use only.

PIK-III

Synonyms: VPS34-IN2

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. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.

PIK-III Chemical Structure

PIK-III Chemical Structure

CAS No. 1383716-40-2

Purity & Quality Control

Batch: S768301 DMSO]63 mg/mL]false]Ethanol]63 mg/mL]false]Water]Insoluble]false Purity: 99.04%
99.04

PIK-III Related Products

Signaling Pathway

Autophagy Signaling Pathways

Autophagy Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U2OS Function assay 2 hrs Inhibition of VPS34 in human U2OS cells incubated for 2 hrs by GFP-FYVE reporter gene assay, IC50=0.012μM 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NCOA4 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of p62 degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NBR1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of NDP52 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
DLD1 Function assay 1 to 10 uM 24 hrs Inhibition of VPS34 in human DLD1 cells assessed as prevention of FTH1 protein degradation at 1 to 10 uM incubated for 24 hrs by Western blot analysis 26819669
VERO-E6 Toxicity assay 48 hrs Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=2.11μM ChEMBL
VERO-E6 Function assay 48 hrs Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging, IC50=7.92μM ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description 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. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
Targets
Vps34 [1]
(Cell-free assay)		 PI3Kδ [1]
(Cell-free assay)
0.018μM 1.2μM
In vitro
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 319.36 Formula

C17H17N7
CAS No. 1383716-40-2 SDF Download PIK-III SDF
Smiles C1CC1CC2=NC(=NC=C2C3=NC(=NC=C3)NC4=CC=NC=C4)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (197.26 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 63 mg/mL

Water : Insoluble


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