Cat. No.: HY-133916

G140

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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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Pureté: 99.17%
CAS No.: 2369751-07-3
Formule: C₁₇H₁₆Cl₂N₄O₂
Masse moléculaire:379.24

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

G140 Chemical Structure

CAS No.: 2369751-07-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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 μM 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 μM 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 μM 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.

Chemical Information

CAS No. 2369751-07-3
Appearance Solid
Masse moléculaire 379.24
Formule C₁₇H₁₆Cl₂N₄O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

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Nature

STING agonist-based ER-targeting molecules boost antigen cross-presentation. [Abstract]

2025 May;641(8061):202-210. PMID: 40140567
Nat Commun

TRABID inhibition activates cGAS/STING-mediated anti-tumor immunity through mitosis and autophagy dysregulation. [Abstract]

2023 May 26;14(1):3050. PMID: 37237031
Adv Sci (Weinh)

PVC Nanoplastics Exposure Exacerbates Asthma through R-Loop Accumulation and Subsequent STING Activation in Macrophages. [Abstract]

2025 Sep 8:e02223. PMID: 40919700

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).
Cell Rep

The N-degron pathway mediates the autophagic degradation of cytosolic mitochondrial DNA during sterile innate immune responses. [Abstract]

2024 Dec 21;44(1):115094. PMID: 39709605

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.
Pharmacol Rep

Pretreatment with alendronate augments lipid A-induced IFN-β production via upregulation of cGAS expression. [Abstract]

2025 Aug 14. PMID: 40810765
bioRxiv

It's Not Rewarding for Mitochondria: Dopamine-Induced Mitochondrial Dysfunction Activates cGAS-STING to Drive IL-6 Secretion in Macrophages. [Abstract]

2026 Apr 25:2026.04.23.719926. PMID: 42079251
bioRxiv

Heterochromatin fidelity is a therapeutic vulnerability in lymphoma and other human cancers. [Abstract]

2025 Feb 5:2025.01.31.635709. PMID: 39975048

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6369 mL

13.1843 mL

26.3685 mL

5 mM

0.5274 mL

2.6369 mL

5.2737 mL

10 mM

0.2637 mL

1.3184 mL

2.6369 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lama L, et, al. Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat Commun. 2019 May 21; 10(1): 2261. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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G140

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Pattern Recognition Receptors Library

Publications Citing Use of MedChemExpress (MCE) G140

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

G140

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Pattern Recognition Receptors Library

Publications Citing Use of MedChemExpress (MCE) G140

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

G140 Related Classifications

HY-133916 Related Classifications