Home Metabolism cGAS inhibitor G150 For research use only.

G150

G150 is a potent and highly selective human cyclic GMP-AMP synthase (cGAS) inhibitor with IC50 of 10.2 nM.

G150 Chemical Structure

G150 Chemical Structure

CAS No. 2369751-30-2

Purity & Quality Control

G150 Related Products

Biological Activity

Description G150 is a potent and highly selective human cyclic GMP-AMP synthase (cGAS) inhibitor with IC50 of 10.2 nM.
Targets
h-cGAS [1]
(Cell-free assay)
10.2 nM
In vitro
In vitro

The most potent h-cGAS-specific derivative with 2-amino pyridine (G150) shows inhibitory activity in THP1 cells and primary human macrophages while a complete absence of off-target effect on a diverse range of sensors. G150 also shows no substantial cellular toxicity[1].
Cell Research Cell lines THP1 cells, primary macrophage cells
Concentrations 10 μM and 5 μM
Incubation Time 1 h
Method

Cellular activation of cGAS enzyme leads to IFNB1 mRNA expression in THP1, and primary human macrophage cells and is quantified using qRT-PCR. Total RNA is isolated from 5 × 105 THP1 cells per well of a 12-well plate, which are pre-incubated with G150 for 1 h. Human primary macrophages are used at 3×105 cells per well of a 12-well plate.

Chemical Information & Solubility

Molecular Weight 391.25 Formula

C18H16Cl2N4O2
CAS No. 2369751-30-2 SDF --
Smiles C1CN(CC2=C1NC3=C2C(=CC(=C3Cl)Cl)C4=CN=C(C=C4)N)C(=O)CO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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