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PIK-III

Cat. No. M8998
PIK-III Structure
Synonym:

VPS34-IN2; Vps34-PIK-III

Size Price Availability Quantity
5mg USD 160 In stock
10mg USD 255 In stock
50mg USD 1050 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PIK-III is a VPS34 inhibitor which blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis. It has IC50 values of 18 nM and 1.2 μM for VPS34 and PI(3)Kδ, respectively. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, and leads to the stabilization of autophagy substrates. 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. Treatment with Vps34-PIK-III leads to an increase in the levels of LC3-I in H4 and PSN1 cells.

Protocol
Cell Experiment
Cell lines H4 cells/ HeLa cells
Preparation 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.
Concentrations 2.5μM in H4 cells/5μM in Hela cells
Incubation time overnight for H4 cells/12h for Hela cells
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 319.36
Formula C17H17N7
CAS Number 1383716-40-2
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.
Honda A, et al. ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. PMID: 26819669.

Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo.
Dowdle WE, et al. Nat Cell Biol. 2014 Nov;16(11):1069-79. PMID: 25327288.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PIK-III, VPS34-IN2; Vps34-PIK-III supplier, PI3K, inhibitors

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