Home Tools
Log in
Cart

Vps34-PIK-III

Catalog No. T6945   CAS 1383716-40-2
Synonyms: PIK-III, VPS34-IN2

Vps34-PIK-III (VPS34-IN2), a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Vps34-PIK-III Chemical Structure
Vps34-PIK-III, CAS 1383716-40-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 47.00
2 mg In stock $ 65.00
5 mg In stock $ 118.00
10 mg In stock $ 213.00
25 mg In stock $ 477.00
50 mg In stock $ 698.00
100 mg In stock $ 993.00
500 mg In stock $ 1,990.00
1 mL * 10 mM (in DMSO) In stock $ 118.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 98.43%
Purity: 98.21%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Vps34-PIK-III (VPS34-IN2), a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.
Targets&IC50 Vps34:0.018μM, PI3Kδ: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].
In vivo The DFX-induced NCOA4-dependent turnover of FTH1 and FTL is blocked with PIK-III which suggests an autophagy-dependent process[2].
Kinase Assay In vitro tyrosine kinase assays.: Assay of IGF-1R-catalyzed substrate phosphorylation of pTG, using a 96-well plate tyrosine kinase assay kit, is performed. We use recombinant epidermal growth factor receptor, immunoprecipitated IR from HEPG2, immunoprecipitated IGF-1R from P6 cells, and IGF-1R immunodepleted supernatant from P6 (representing "non-IGF-1R tyrosine kinases"). After 30-min treatment of the receptors with the desired compounds in the kinase buffer [50 mM HEPES buffer (pH 7.4), 20 mM MgCl2, 0.1 MnCl2, and 0.2 Na3VO4], the kinase reaction is activated by addition of ATP. The phosphorylated polymer substrate is probed with a phosphotyrosine-specific monoclonal antibody conjugated to horseradish peroxidase, clone PT-66. Color is developed with horseradish peroxidase chromogenic substrate O-phenylenediamine dihydrochloride and quantitated by spectrophotometry (ELISA reader). IGF-1R tyrosine autophosphorylation is analyzed by a sandwich ELISA assay. Briefly, 96-well plates are coated overnight at 4°C with 1 μg/well of an antibody to IGF-1R β-subunit. The plates are blocked with 1% BSA in PBS Tween for 1 h, and then 80 μg/well of total protein lysate from the P6 cell line is added. As a negative control we use total protein lysate from the R- cell line. The investigated compounds are added in tyrosine kinase buffer without ATP at room temperature for 30 min before kinase activation with ATP. Kinase assay is performed using the Sigma kit (see above). After spectrophotometry the IC50 values of inhibitors are determined using the REGRESSION function of Statistica program.
Cell Research 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)
Synonyms PIK-III, VPS34-IN2
Molecular Weight 319.36
Formula C17H17N7
CAS No. 1383716-40-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 59 mg/mL (184.7 mM)

Ethanol: 59 mg/mL (184.7 mM)

TargetMolReferences and Literature

1. Honda A, et al. Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo. ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. 2. Dowdle WE, et al. Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat Cell Biol. 2014 Nov;16(11):1069-79.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library Neural Regeneration Compound Library Immuno-Oncology Compound Library Stem Cell Differentiation Compound Library Metabolism Compound Library Reprogramming Compound Library Bioactive Compound Library PI3K-AKT-mTOR Compound Library Inhibitor Library HIF-1 Signaling Pathway Compound Library

Related Products

Related compounds with same targets
LC3-mHTT-IN-AN1 Brazilin Flavopiridol MHY1485 Quercetin Autocamtide-2-related inhibitory peptide, myristoylated acetate(201422-04-0 free base) EACC SB 216763

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Vps34-PIK-III 1383716-40-2 Autophagy PI3K/Akt/mTOR signaling PI3K Vps34 PIK III Vps-34-PIK-III Inhibitor PIK-III Phosphoinositide 3-kinase Vps34PIKIII VPS34-IN2 inhibit inhibitor

 

TargetMol