2. PI3K/Akt/mTOR Autophagy
  3. PI3K Autophagy
  4. Vps34-IN-1

Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns(3)P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy.

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CAS 番号 : 1383716-33-3

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10 mM * 1 mL in DMSO
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 USD 121 在庫あり
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10 mM * 1 mL in DMSO USD 121 在庫あり
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5 mg $110 在庫あり
10 mg $176 在庫あり
25 mg $330 在庫あり
50 mg $495 在庫あり
100 mg $715 在庫あり
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カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Vps34-IN-1 関連抗体

Top Publications Citing Use of Products

    Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

    VPS34-IN-1, VPS34-IN-2, PIK-III, and SAR405 (all 1 μM, 48 h) exhibited similar inhibition of 0.02 MOI WT SARS-CoV-2 infection in Vero E6 cells.

    Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

    VPS34-IN-1, VPS34-IN-2, PIK-III, and SAR405 (all 1 μM, 48 h) protected cells from SARS-CoV-2-induced CPE, highlighting the critical role of VPS34 in SARS-CoV-2 infection.

    Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

    Pharmacological profiling of VPS34 inhibitors against SARS-CoV-2 variants demonstrated that the EC50 of VPS34-IN-1 was 0.36, 0.99, 0.46, and 0.24 μM against WT, Beta, Delta, and Omicron variants, respectively.

    Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec 18.

    Cytotoxicity assessments at 48 h in Vero E6 cells revealed that the CC50 values of VPS34-IN-1 was 11.00 μM.

    Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.  [Abstract]

    Huh7 and MHCC97H cells are treated with VPS34-IN1 for 24 h, and cell lysates are subjected to western blot analysis with the indicated antibodies.

    Vps34-IN-1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525.  [Abstract]

    PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.

    PI3K アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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    • 純度とドキュメンテーション

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    製品説明

    Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns(3)P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy[1][2][3].

    IC50 & Target[1]

    Vps34

    25 nM (IC50)

    体外実験

    Vps34-IN-1 does not significantly inhibit any of the lipid kinases including class I (p110α, p110β p110γ and p110δ) and all three members of the class II PI3Ks (PI3KC2α, PI3KC2β and PI3KC2γ) enzymes[1].
    Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) inhibits PtdIns(3)P levels at endosomes in a dose-dependent manner[1].
    Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) induces a dose-dependent reduction in SGK3 activity that is maximally lowered by ~60% at 1 μM and ~40% at 0.1 μM. The suppression of SGK3 activity is accompanied by a commensurate decrease in T-loop and hydrophobic motif phosphorylation[1].
    Vps34-IN-1 (1, 2, 4 μM; 24 h) induces a dose-dependent inhibition of SGK3 phosphorylation[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Vps34-IN-1 関連抗体

    Western Blot Analysis[2]

    Cell Line: MHH97H and Huh7 cells
    Concentration: 1, 2, 4 μM
    Incubation Time: 24 h
    Result: Induced a dose-dependent inhibition of SGK3 phosphorylation in MHH97H and Huh7 cells.
    Reduced the expression of CSC-related markers CD133 and Nanog.
    分子量

    425.91

    分子式

    C21H24ClN7O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)(O)CNC1=NC=C(C2=CC=NC(NC3=CC=NC(Cl)=C3)=N2)C(CC4CC4)=N1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 31 mg/mL (72.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3479 mL 11.7396 mL 23.4791 mL
    5 mM 0.4696 mL 2.3479 mL 4.6958 mL
    10 mM 0.2348 mL 1.1740 mL 2.3479 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    純度とドキュメンテーション

    純度: 99.79%

    COA (254 KB) HNMR (285 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3479 mL 11.7396 mL 23.4791 mL 58.6978 mL
    5 mM 0.4696 mL 2.3479 mL 4.6958 mL 11.7396 mL
    10 mM 0.2348 mL 1.1740 mL 2.3479 mL 5.8698 mL
    15 mM 0.1565 mL 0.7826 mL 1.5653 mL 3.9132 mL
    20 mM 0.1174 mL 0.5870 mL 1.1740 mL 2.9349 mL
    25 mM 0.0939 mL 0.4696 mL 0.9392 mL 2.3479 mL
    30 mM 0.0783 mL 0.3913 mL 0.7826 mL 1.9566 mL
    40 mM 0.0587 mL 0.2935 mL 0.5870 mL 1.4674 mL
    50 mM 0.0470 mL 0.2348 mL 0.4696 mL 1.1740 mL
    60 mM 0.0391 mL 0.1957 mL 0.3913 mL 0.9783 mL
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    Vps34-IN-1 Related Classifications

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    Keywords:

    Vps34-IN-11383716-33-3PI3KAutophagyPhosphoinositide 3-kinaseclass III PI3KPtdInsVps34-Vps15SGK3PtdIns(3)PT-loophydrophobic motifsInhibitorinhibitorinhibit

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    製品番号:
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