Art. -Nr.: HY-128583

G150

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC₅₀ of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory.

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Reinheit: 99.20%
CAS. Nr.: 2369751-30-2
Formel: C₁₈H₁₆Cl₂N₄O₂
Molecular Weight:391.25

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

G150 Chemical Structure

CAS. Nr.: 2369751-30-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 10.2 nM (h-cGAS)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	IC₅₀	<1 μM Compound: 51; G150	Cytotoxicity against mouse RAW264.7 cells assessed as cell growth inhibition measured after 24 hrs by Celltiter-Glo assay Cytotoxicity against mouse RAW264.7 cells assessed as cell growth inhibition measured after 24 hrs by Celltiter-Glo assay	[PMID: 33984476]
THP-1	IC₅₀	1.96 μM Compound: 51; G150	Cytotoxicity against human THP-1 cells assessed as cell growth inhibition measured after 24 hrs by Celltiter-Glo assay Cytotoxicity against human THP-1 cells assessed as cell growth inhibition measured after 24 hrs by Celltiter-Glo assay	[PMID: 33984476]
THP-1	IC₅₀	1.96 μM Compound: 6; G150	Cytotoxicity against human THP-1 cells assessed as cell growth inhibition Cytotoxicity against human THP-1 cells assessed as cell growth inhibition	[PMID: 34044539]

In Vitro

G150 (0.1-100 μM; 1 h) affects IFNB1 and CXCL10 expression in human THP1 cells and primary human macrophages^[1].
G150 (5-10 μM; 1 h) affects dsDNA sensing in THP1 cells and primary human macrophages^[1].
G150 (0.1-100 μM; 1 h) affects the NF-κB pathway activation in THP1-Dual cells^[1].

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

RT-PCR^[1]

Cell Line:

Human THP1 cells and primary human macrophages
Concentration:

0.1-100 μM
Incubation Time:

1 hour
Result:

Dose-dependently inhibited IFNB1 and interferon-stimulated genes monitoring CXCL10 expression with IC₅₀s of 1.96 and 7.57 μM respectively in human THP1 cells, and inhibited IFNB1 and CXCL10 expression with IC₅₀s of 0.62 and 0.87 μM respectively in primary human macrophages.

RT-PCR^[1]

Cell Line:

Human THP1 cells and primary human macrophages
Concentration:

5 and 10 μM
Incubation Time:

1 hour
Result:

Inhibited dsDNA sensing with a concentration of 10 μM in THP1 cells and with a concentration of 5 μM in primary human macrophages.

RT-PCR^[1]

Cell Line:

THP1-Dual cells
Concentration:

0.1-100 μM
Incubation Time:

1 hour
Result:

Inhibited SEAP activity and luciferase activity with IC₅₀s of 0.90 and 1.79 μM respectively in THP1-Dual cells.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2369751-30-2
Appearance Solid
Molecular Weight 391.25
Formel C₁₈H₁₆Cl₂N₄O₂
Color White to off-white
SMILES

NC1=CC=C(C2=C3C(NC4=C3CN(C(CO)=O)CC4)=C(Cl)C(Cl)=C2)C=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

Mol Cell

Cytosolic DNA sensing by cGAS/STING promotes TRPV2-mediated Ca2+ release to protect stressed replication forks. [Abstract]

2023 Jan 14;S1097-2765(22)01217-5. PMID: 36696898
Nat Commun

2026 May 27. PMID: 42203763
Adv Sci (Weinh)

Oleic Acid Dissolves cGAS-DNA Phase Separation to Inhibit Immune Surveillance. [Abstract]

2023 May;10(14):e2206820. PMID: 36950761
Cell Death Dis

Airway epithelial cGAS inhibits LPS-induced acute lung injury through CREB signaling. [Abstract]

2023 Dec 19;14(12):844. PMID: 38114479
EMBO J

Basal IFN-λ2/3 expression mediates tight junction formation in human epithelial cells. [Abstract]

2025 Sep 1. PMID: 40890487
J Transl Med

Blockade of the mitochondrial DNA release ameliorates hepatic ischemia-reperfusion injury through avoiding the activation of cGAS-Sting pathway. [Abstract]

2024 Aug 28;22(1):796. PMID: 39198913
Int Immunopharmacol

Quercetin alleviates LPS-induced inflammation and immunosuppression in broiler spleen via regulating the mtDNA/cGAS/STING axis. [Abstract]

2026 May 1:176:116482. PMID: 41797087
Toxicol Appl Pharmacol

Activation of the cGAS-STING pathway in monocytes exacerbates pulmonary fibrosis induced by paraquat poisoning. [Abstract]

2025 Aug 9:504:117502. PMID: 40789441

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (255.59 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

2.5559 mL

12.7796 mL

25.5591 mL

5 mM

0.5112 mL

2.5559 mL

5.1118 mL

10 mM

0.2556 mL

1.2780 mL

2.5559 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (5.32 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 (5.32 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 (5.32 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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)
Handling Instructions (2659 KB)

Verweise

[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, 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	2.5559 mL	12.7796 mL	25.5591 mL	63.8978 mL
	5 mM	0.5112 mL	2.5559 mL	5.1118 mL	12.7796 mL
	10 mM	0.2556 mL	1.2780 mL	2.5559 mL	6.3898 mL
	15 mM	0.1704 mL	0.8520 mL	1.7039 mL	4.2599 mL
	20 mM	0.1278 mL	0.6390 mL	1.2780 mL	3.1949 mL
	25 mM	0.1022 mL	0.5112 mL	1.0224 mL	2.5559 mL
	30 mM	0.0852 mL	0.4260 mL	0.8520 mL	2.1299 mL
	40 mM	0.0639 mL	0.3195 mL	0.6390 mL	1.5974 mL
	50 mM	0.0511 mL	0.2556 mL	0.5112 mL	1.2780 mL
	60 mM	0.0426 mL	0.2130 mL	0.4260 mL	1.0650 mL
	80 mM	0.0319 mL	0.1597 mL	0.3195 mL	0.7987 mL
	100 mM	0.0256 mL	0.1278 mL	0.2556 mL	0.6390 mL

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G150

Immunology/Inflammation Compound Library

Targeted Diversity 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) G150

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

G150

Immunology/Inflammation Compound Library

Targeted Diversity 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) G150

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

G150 Related Classifications

HY-128583 Related Classifications