G150

Catalog No.S8944 Batch:S894401

Technical Data

Formula	C₁₈H₁₆Cl₂N₄O₂
Molecular Weight	391.25	CAS No.	2369751-30-2
Solubility (25°C)*	In vitro	DMSO	78 mg/mL (199.36 mM)
		Ethanol	2 mg/mL (5.11 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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].

Protocol (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

[1] Lama L, et al. Nat Commun. 2019 May 21;10(1):2261.

Selleck's G150 has been cited by 4 publications

Polystyrene microplastics induce pulmonary fibrosis by promoting alveolar epithelial cell ferroptosis through cGAS/STING signaling [ Ecotoxicol Environ Saf, 2024, 277:116357]	PubMed: 38677073
Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway [ Virus Res, 2024, 343:199344]	PubMed: 38431054
A novel TREX1 inhibitor, VB-85680, upregulates cellular interferon responses [ PLoS One, 2024, 19(8):e0305962]	PubMed: 39178223
HIV-1-induced type I IFNs promote viral latency in macrophages [ J Leukoc Biol, 2022, 10.1002/JLB.4MA0422-616R]	PubMed: 35588262

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.