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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- No. CAS: 2369750-66-1
- Fòrmula: C16H14Cl2N4O2
- Peso molecular:365.21
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
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.
Chemical Information
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No. CAS 2369750-66-1
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Peso molecular 365.21
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Fòrmula C16H14Cl2N4O2
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SMILES
O=C(N1CC=2C=3C(=CC(Cl)=C(Cl)C3NC2CC1)C=4C=NNC4)CO
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
cGAS-IN-9 Related Classifications
HY-147129 Related Classifications
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Keywords
- cGAS-IN-9
- 2369750-66-1
- Guanylate Cyclase
- Adenylate Cyclase
- CXCR
- NF-κB
- Adenylyl cyclase
- CXC chemokine receptors
- C-X-C motif chemokine receptors
- Nuclear factor-κB
- Nuclear factor-kappaB
- ATP
- human immune cells
- CXCL10 mRNA
- h-cGAS
- GTP
- IFNB1 mRNA
- STING pathway
- human cyclic GMP-AMP synthase
- human cells
- NF-κB pathway
- Inhibitor
- inhibitor
- inhibit