2. Cell Cycle/DNA Damage
  3. Eukaryotic Initiation Factor (eIF)
  4. GCN2-IN-1

GCN2-IN-1 (A-92) est un inhibiteur puissant de la kinase 2 non réprimable (GCN2) avec un IC50 de <0,3 μM dans le dosage enzymatique et un IC50 de 0,3-3 μM dans le dosage cellulaire.

GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.

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

CAS No. : 1448693-69-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 25 publication(s) in Google Scholar

GCN2-IN-1 Related Antibodies

Top Publications Citing Use of Products

    GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2025 Nov;27(11):1889-1901.  [Abstract]

    Ubiquitylation of whole-cell proteins and OMM proteins of cells cultured in medium supplemented with 0 mM or 1 mM Leu and/or 0 µM or 10 µM GCN2-IN-1 for 3 h. For each sample, 10 µg proteins were loaded. Ubiquitylation levels were normalized to the total OMM protein amount.

    GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2024 May 22;52(9):5356-5375.  [Abstract]

    U2OS cells were treated with a PERK inhibitor (GSK II, 40 μM), or with GCN2-IN-1 (4 μM), for 3 h prior to transfection. mRNA (1 μg) encoding GFP (green) was transfected, and cells were fixed 1.5 h post-transfection. Cells were stained using anti-G3BP1 (magenta).

    GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 25;14(1):6777.  [Abstract]

    MDA-MB 231 cells were cultured for 72 hours in complete medium (CM) and medium containing 25% amino acids (low amino acid). Then, they were treated with (+) or (-) 1 μM GCN2-IN-1 for 72 hours, respectively, and Western blot analysis was performed to detect the expression of the proteins shown.

    GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 8;14(1):5535.  [Abstract]

    After treating HeLa cells with the GCN2 inhibitor GCN2-IN-1 (A92) at progressively increasing concentrations for 5 hours, the specified proteins in the lysate were analyzed by immunoblotting.

    GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jul;30(7):1666-1678.  [Abstract]

    Immunoblotting of phosphorylated eIF2a (ser51) following treatment of A549 with CuET (2 h) +/–PERK inhibitor combined with siRNA against HRI or GCN2-IN-1 (10 μM; 30 min). Numbers below the blot indicate the signal ratio p-eIF2a/β-actin.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay[1].

    IC50 & Target

    eIF2

     

    In Vitro

    GCN2-IN-1 (Compound A-92) is a GCN2 inhibitor, which may be useful as a chemotherapeutic drug for the treatment of cancer[1].

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

    GCN2-IN-1 Related Antibodies
    Molecular Weight

    402.41

    Formula

    C19H18N10O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    C1(NC2=CN(C3CCOCC3)N=C2)=NC=C(N=NN4C5=CC6=C(C=C5)C=NN6)C4=N1
    Shipping

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

    DMSO : 50 mg/mL (124.25 mM; Need ultrasonic; 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 2.4850 mL 12.4251 mL 24.8503 mL
    5 mM 0.4970 mL 2.4850 mL 4.9701 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.21 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.
    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: 99.46%

    SDS (393 KB)

    COA (250 KB) HNMR (282 KB) RP-HPLC (254 KB) LCMS (97 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4850 mL 12.4251 mL 24.8503 mL 62.1257 mL
    5 mM 0.4970 mL 2.4850 mL 4.9701 mL 12.4251 mL
    10 mM 0.2485 mL 1.2425 mL 2.4850 mL 6.2126 mL
    15 mM 0.1657 mL 0.8283 mL 1.6567 mL 4.1417 mL
    20 mM 0.1243 mL 0.6213 mL 1.2425 mL 3.1063 mL
    25 mM 0.0994 mL 0.4970 mL 0.9940 mL 2.4850 mL
    30 mM 0.0828 mL 0.4142 mL 0.8283 mL 2.0709 mL
    40 mM 0.0621 mL 0.3106 mL 0.6213 mL 1.5531 mL
    50 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2425 mL
    60 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0354 mL
    80 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7766 mL
    100 mM 0.0249 mL 0.1243 mL 0.2485 mL 0.6213 mL
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    GCN2-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:

    GCN2-IN-11448693-69-3Eukaryotic Initiation Factor (eIF)Inhibitorinhibitorinhibit

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