2. Autophagy
  3. Autophagy
  4. AS1842856

AS1842856, un inhibiteur spécifique de Foxo1 (IC50=30 nM), supprime puissamment l'autophagie[1 ]. AS1842856 inhibe l'activité de FoxO1 en supprimant l'expression de SIRT1. AS1842856 ne réduit l'activité de FoxO1 qu'en se liant à lui, sans affecter sa transcription et son expression protéique.

AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy. AS1842856 reduces Foxo1 activity and, to a lesser extent, inhibits Foxo1 protein expression by simply binding to Foxo1.

For research use only. We do not sell to patients.

AS1842856 Chemical Structure

AS1842856 Chemical Structure

CAS No. : 836620-48-5

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Customer Review

Based on 60 publication(s) in Google Scholar

AS1842856 Related Antibodies

Top Publications Citing Use of Products

59 Publications Citing Use of MCE AS1842856

WB

    AS1842856 purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2022 Nov 24.  [Abstract]

    AS1842856 (1 μM; 48 h) reverses CEP55 downregulation-mediated inhibition of PCNA and CDK2 levels and elevation of cl-caspase-3 expression in Ishikawa and RL95-2 cells.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy[1]. AS1842856 reduces Foxo1 activity and, to a lesser extent, inhibits Foxo1 protein expression by simply binding to Foxo1[2].

    IC50 & Target

    IC50: 30 nM (Foxo1)[1]
    In Vitro

    AS1842856 potently inhibits human Foxo1 transactivation and reduces glucose production through the inhibition of glucose-6 phosphatase and phosphoenolpyruvate carboxykinase mRNA levels in a rat hepatic cell line[1]. After AS1842856 treatment, there is no significant difference in the protein expression of p-FoxO1 and FoxO1 compared with the control group, but the expression of p-Akt is decreased compared with the control group[2].

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

    AS1842856 Related Antibodies
    In Vivo

    Oral administration of AS1842856 to diabetic db/db mice leads to a drastic decrease in fasting plasma glucose level via the inhibition of hepatic gluconeogenic genes, whereas administration to normal mice has no effect on the fasting plasma glucose level. Treatment with AS1842856 also suppresses an increase in plasma glucose level caused by pyruvate injection in both normal and db/db mice[1].

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

    347.38

    Formula

    C18H22FN3O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(C1=CN(CC)C2=C(C(N)=C(F)C(NC3CCCCC3)=C2)C1=O)O
    Shipping

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

    DMSO : 5 mg/mL (14.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8787 mL 14.3935 mL 28.7869 mL
    5 mM 0.5757 mL 2.8787 mL 5.7574 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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    90% Corn Oil

      Solubility: ≥ 1.67 mg/mL (4.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

      Solubility: 1 mg/mL (2.88 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  6% HP-β-CD in Saline

      Solubility: 10 mg/mL (28.79 mM); Suspension solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC/saline water

      Solubility: 2 mg/mL (5.76 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.88%

    SDS (537 KB)

    COA (248 KB) RP-HPLC (245 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Rat hepatoma Fao cells are cultured in DMEM with 5.5 mM glucose and 10% FBS. Glucose production rate is measured using glucose CII-test reagent. In brief, after 18 h of treatment with AS1842856 at the indicated concentrations, the cells are ished three times with PBS. The cells are then incubated for 3 h at 37°C in 5% CO2 in a glucose production buffer (glucose-free DMEM, pH 7.4, containing 20 mM sodium pyruvate, without phenol red)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    AS1842856 is dissolved in 6% cyclodextrin for oral administration. Pyruvate or glucose tolerance tests are performed in male mice aged 7 to 9 weeks. Mice are orally administered either AS1842856 dissolved in 6% cyclodextrin or vehicle (6% cyclodextrin only) at three time points (8 AM, 6 PM, and 8 AM on the second day). Food is removed after initial dosing and withheld throughout the study (26-h fasting)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8787 mL 14.3935 mL 28.7869 mL 71.9673 mL
    5 mM 0.5757 mL 2.8787 mL 5.7574 mL 14.3935 mL
    10 mM 0.2879 mL 1.4393 mL 2.8787 mL 7.1967 mL
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    AS1842856 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:

    AS1842856836620-48-5AS 1842856AS-1842856AutophagyInhibitorinhibitorinhibit

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