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^[1].

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.

365.21

C₁₆H₁₄Cl₂N₄O₂

2369750-66-1

O=C(N1CC=2C=3C(=CC(Cl)=C(Cl)C3NC2CC1)C=4C=NNC4)CO

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• [1]. Lama L, et al. Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression. Nat Commun. 2019;10(1):2261. Published 2019 May 21.  [Content Brief]