1. Immunology/Inflammation
  2. Cyclic GMP-AMP Synthase
  3. G140

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.

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No. CAS : 2369751-07-3

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
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10 mg En stock
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Revisión del cliente

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    G140 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 8:e02223.  [Abstract]

    Effects of pharmacological inhibition or gene knockout of the cGAS-STING pathway on PVC NPs-induced phosphorylation of TBK1 and IRF3 cGAS inhibitor (G140, 2 µM).

    G140 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 8:e02223.  [Abstract]

    The relative mRNA expression levels of pro-inflammatory cytokines (TNF-α) in STING KO cells treated with the cGAS inhibitor (G140, 2 µM).

    G140 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Dec 21;44(1):115094.  [Abstract]

    Immunoblotting analysis of HeLa cells treated with 10 μM G140, 10 μM H151, or 10 μM NU7441 for 18 h in the presence of 1 μg/mL poly(dA:dT).

    G140 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Dec 21;44(1):115094.  [Abstract]

    The mRNA expression relative to GAPDH was measured by RT-qPCR. RNAs were isolated from HeLa cells treated with MG132 or co-treated with MG132 and G140 or H151 for 12 h.
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    Descripciòn

    G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity[1].

    IC50 & Target

    cGAS

     

    Cellular Effect
    Cell Line Type Value Description References
    H69AR IC50
    2.69 3
    Compound: 5; G140
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    [PMID: 34044539]
    H69AR IC50
    2.69 3
    Compound: 5; G140
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    [PMID: 34044539]
    H69AR IC50
    2.69 3
    Compound: 5; G140
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    [PMID: 34044539]
    THP-1 IC50
    1.7 3
    Compound: 5; G140
    Cytotoxicity against human THP-1 cells assessed as cell growth inhibition
    Cytotoxicity against human THP-1 cells assessed as cell growth inhibition
    [PMID: 34044539]
    THP1-Dual CC50
    > 50 3
    Compound: 5; G140
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    [PMID: 34044539]
    THP-1 IC50
    1.7 3
    Compound: 5; G140
    Cytotoxicity against human THP-1 cells assessed as cell growth inhibition
    Cytotoxicity against human THP-1 cells assessed as cell growth inhibition
    [PMID: 34044539]
    THP1-Dual CC50
    >50 3
    Compound: 5; G140
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    [PMID: 34044539]
    THP1-Dual CC50
    > 50 3
    Compound: 5; G140
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    [PMID: 34044539]
    In Vitro

    G140 (0.1-100 μM; 4 h) inhibits h-cGAS in a dose-dependent manner with IC50s of 1.70 and 0.86 μM in human THP1 and primary macrophages, respectively[1].
    G140 (0.1-100 μM; 24 h) inhibits cells viability with a LD50 of >100 μM in THP1 cells[1].

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

    Peso molecular

    379.24

    Fòrmula

    C17H16Cl2N4O2

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OCC(N(C1)CCC(N2)=C1C3=C2C(Cl)=C(Cl)C=C3C4=NN(C)C=C4)=O

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvente y solubilidad
    In Vitro: 

    DMSO : 250 mg/mL (659.21 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 2.6369 mL 13.1843 mL 26.3685 mL
    5 mM 0.5274 mL 2.6369 mL 5.2737 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.

    • Calculadora de molaridad

    • Calculadora de dilución

    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: ≥ 2.08 mg/mL (5.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
    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.
    Pureza y Documentación
    Referencias

    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 2.6369 mL 13.1843 mL 26.3685 mL 65.9213 mL
    5 mM 0.5274 mL 2.6369 mL 5.2737 mL 13.1843 mL
    10 mM 0.2637 mL 1.3184 mL 2.6369 mL 6.5921 mL
    15 mM 0.1758 mL 0.8790 mL 1.7579 mL 4.3948 mL
    20 mM 0.1318 mL 0.6592 mL 1.3184 mL 3.2961 mL
    25 mM 0.1055 mL 0.5274 mL 1.0547 mL 2.6369 mL
    30 mM 0.0879 mL 0.4395 mL 0.8790 mL 2.1974 mL
    40 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6480 mL
    50 mM 0.0527 mL 0.2637 mL 0.5274 mL 1.3184 mL
    60 mM 0.0439 mL 0.2197 mL 0.4395 mL 1.0987 mL
    80 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL
    100 mM 0.0264 mL 0.1318 mL 0.2637 mL 0.6592 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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    Inquiry Information

    Nombre del producto:
    G140
    Cat. No.:
    HY-133916
    Cantidad:
    MCE Japan Authorized Agent: