Home Autophagy Autophagy inhibitor - PI3K inhibitor - LC3 inhibitor PIK-III

research use only

PIK-III Autophagy inhibitor

Cat.No.S7683

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 Autophagy inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 319.36

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight 319.36 Formula

C17H17N7

 Storage (From the date of receipt)
CAS No. 1383716-40-2 Download SDF Storage of Stock Solutions

Synonyms VPS34-IN2 Smiles C1CC1CC2=NC(=NC=C2C3=NC(=NC=C3)NC4=CC=NC=C4)N

Solubility

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Vps34 [1]
(Cell-free assay)
0.018μM
PI3Kδ [1]
(Cell-free assay)
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, this compound 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, it inhibits the clearance of mitochondria.This chemical treatment leads to an increase in the levels of LC3-I in H4 and PSN1 cells. In Panc10.05 cells, this inhibitor increases the levels of LC3-II in parallel with LC3-I suggesting a cell type-specific response[1].
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map