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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Vps34-IN-1 Chemical Structure

Vps34-IN-1 Chemical Structure

CAS No. : 1383716-33-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 34 In-stock
5 mg USD 110 In-stock
10 mg USD 176 In-stock
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100 mg USD 715 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Vps34-IN-1 Related Antibodies

Top Publications Citing Use of Products

    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.

    View All PI3K Isoform Specific Products:

    View All Isoforms
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    In Vitro

    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 Related Antibodies

    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.
    Molecular Weight

    425.91

    Formula

    C21H24ClN7O
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    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
    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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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • 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.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.79%

    COA (254 KB) HNMR (286 KB) LCMS (106 KB)

    Handling Instructions (2659 KB)
    References

    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

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

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

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