Vps34 inhibitor PIK-III

SKU: orb1226398

Description

Vps34 inhibitor PIK-III (PIK-III) is a potent, selective inhibitor of Vps34 with IC50 of 18 nM, shows >100-fold selectivity over other class I PI3Ks, PI4Kβ and mTOR; inhibits the localization of GFP-FYVE in mammalian cells with IC50 of 55 nM, which is >10,000 times more potent than the non-selective VPS34 inhibitor 3-MA; robustly inhibits autophagy and LC3 lipidation, leads to the stabilization of autophagy substrates in mammalian cells.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1383716-40-2
• MW: 319.3638
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₇N₇
• SMILES: NC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1
• Target: PI3K
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• In Vivo:
  Animal model: C57BL/6 mice. Dosage: 10 mg/kg; 2 mg/kg. Administration: Oral administration; intravenous injection.
• In Vitro:
  Cell Viability Assay Cell line: DLD1 cells. Concentration: 1, 5, 10 μM. Incubation time: 24 h. Result: Prevented the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1.RT-PCR Cell line: HCC cells. Concentration: 5 μM. Incubation time: 24 h. Result: Inhibited stemness genes expression. Western blot analysis. Cell line: Huh7 and MHCC97H cells. Concentration: 5 μM. Incubation time: 24 h. Result: Inhibited liver CSCs by activating AMPK.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PIK-III

Quick Database Links

Gene Symbol

PI3K