cGAS-IN-9
cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC50 values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC50 of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases.
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- CAS. Nr.: 2369750-66-1
- Formel: C16H14Cl2N4O2
- Molecular Weight:365.21
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
2.95 μM
Compound: 4; G108
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Cytotoxicity against human THP-1 cells assessed as cell growth inhibition
Cytotoxicity against human THP-1 cells assessed as cell growth inhibition
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[PMID: 34044539] |
In Vitro
cGAS-IN-9 (Compound G108) (5 h) inhibits dsDNA-induced IFNB1 and CXCL10 mRNA expression in THP1 cells, with IC50 values of 2.95 μM and 3.56 μM, respectively[1].
cGAS-IN-9 (5 h) inhibits dsDNA-induced IFNB1 and CXCL10 mRNA expression in primary human macrophages, with IC50 values of 1.53 μM and 0.59 μM, respectively[1].
cGAS-IN-9 (5-10 μM; 5 h) specifically inhibits dsDNA-induced IFNB1 mRNA expression in primary human macrophages at a concentration of 5 μM, while only exhibits weak off-target activity against the cGAMP and hpRNA pathways in THP1 cells at a concentration of 10 μM[1].
cGAS-IN-9 (25 h) inhibits the activation of cGAS-dependent NF-κB and interferon pathways in THP1-Dual cells, with an IC50 of 2.27 μM for NF-κB reporter gene activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 2369750-66-1
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Molecular Weight 365.21
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Formel C16H14Cl2N4O2
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SMILES
O=C(N1CC=2C=3C(=CC(Cl)=C(Cl)C3NC2CC1)C=4C=NNC4)CO
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)