Vps34-PIK-III

SKU: orb1300323

Description

VPS34-IN2 (PIK-III) is a potent and selective VPS34 inhibitor that blocks autophagy, leading to the accumulation of autophagy substrates. It is a valuable chemical tool for studying autophagy mechanisms in both cellular and in vivo models across cancer and neurodegenerative disease research.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1383716-40-2
• MW: 319.36
• Purity: 98.39%
• Formula: C₁₇H₁₇N₇
• SMILES: Nc1ncc(c(CC2CC2)n1)-c1ccnc(Nc2ccncc2)n1
• Target: Autophagy,PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.26 mM);DMSO:60 mg/mL (187.88 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:59 mg/mL (184.74 mM)

Bioactivity

• Target IC50:
  VPS34:0.018μM|PI3Kδ:1.2μM|PI3Kα:3.96 μM|PI3Kγ:3.04 μM
• In Vivo:
  The DFX-induced NCOA4-dependent turnover of FTH1 and FTL is blocked with PIK-III which suggests an autophagy-dependent process.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, PI3K, PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ, Vps34PIKIII, Vps-34-PIK-III, Vps34-PIK-III, Vps34 PIK III, Vps34

Compound Identifiers

PubChem CID

67983123