1. Cell Cycle/DNA Damage Autophagy
  2. Eukaryotic Initiation Factor (eIF) Autophagy
  3. GCN2iB

GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.

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

GCN2iB Chemical Structure

GCN2iB Chemical Structure

CAS No. : 2183470-12-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 275 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GCN2iB purchased from MedChemExpress. Usage Cited in: FASEB J. 2023 Mar;37(3):e22820.  [Abstract]

    GCN2iB (1 μM; 12 h) significantly inhibits Cholic acid (CA)-induced phosphorylation of GCN2 and eIF2α in HTR8/SVneo cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.

    IC50 & Target

    IC50: 2.4 nM (GCN2)[1].

    In Vitro

    GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity[1].

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

    In Vivo

    In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth. Notably, a combination of ASNase and GCN2iB elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect[1].

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

    Molecular Weight

    451.83

    Formula

    C18H12ClF2N5O3S

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=S(C1=CC(Cl)=CN=C1OC)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O

    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 : 50 mg/mL (110.66 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 2.2132 mL 11.0661 mL 22.1322 mL
    5 mM 0.4426 mL 2.2132 mL 4.4264 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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: ≥ 1.67 mg/mL (3.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% Corn Oil

      Solubility: ≥ 1.67 mg/mL (3.70 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.

    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: 99.90%

    References
    Animal Administration
    [1]

    Mice[1]
    A suspension of CCRF-CEM, HPB-ALL, MV-4-11, or SU.86.86 cells (1×107 cells/site) is subcutaneously injected into the right flanks of 6-week-old female SCID mice. Tumor volume is calculated as volume =L×l2×1/2, where L represents the longest diameter across the tumor and l represents the corresponding perpendicular distance. Body weight is also measured. To assess the anti-tumor activity, mice with tumor mass ~200 mm3 are sorted into treatment groups (N=5/group). The tumors are monitored and mice are euthanized when an endpoint is reached, or at the end of the study, whichever comes first. From the next day of randomization, GCN2 inhibitors (e.g., GCN2iB, 10 mpk, twice a day) or ASNase is orally or intraperitoneally administered to mice bearing the xenografts for 7 to 10 days, respectively. T/C (%), an index of anti-tumor activity, is calculated by comparing the mean change in tumor volume during the treatment period in the control and treated groups[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, 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 2.2132 mL 11.0661 mL 22.1322 mL 55.3305 mL
    5 mM 0.4426 mL 2.2132 mL 4.4264 mL 11.0661 mL
    10 mM 0.2213 mL 1.1066 mL 2.2132 mL 5.5331 mL
    15 mM 0.1475 mL 0.7377 mL 1.4755 mL 3.6887 mL
    20 mM 0.1107 mL 0.5533 mL 1.1066 mL 2.7665 mL
    25 mM 0.0885 mL 0.4426 mL 0.8853 mL 2.2132 mL
    30 mM 0.0738 mL 0.3689 mL 0.7377 mL 1.8444 mL
    40 mM 0.0553 mL 0.2767 mL 0.5533 mL 1.3833 mL
    50 mM 0.0443 mL 0.2213 mL 0.4426 mL 1.1066 mL
    60 mM 0.0369 mL 0.1844 mL 0.3689 mL 0.9222 mL
    80 mM 0.0277 mL 0.1383 mL 0.2767 mL 0.6916 mL
    100 mM 0.0221 mL 0.1107 mL 0.2213 mL 0.5533 mL
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    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.

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    Product Name:
    GCN2iB
    Cat. No.:
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