cGAS inhibitor 36

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Chemical Structure : cGAS inhibitor 36

Catalog No.: PC-23640Not For Human Use, Lab Use Only.

cGAS inhibitor 36 is a potent, orally bioavailable inhibitor of cyclic GMP-AMP synthase (cGAS) with biochemical IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

cGAS inhibitor 36 is a potent, orally bioavailable inhibitor of cyclic GMP-AMP synthase (cGAS) with biochemical IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS respectively.
cGAS inhibitor 36 shows cellular activity with a THP1 cGAMP cell assay with IC50 of 60 nM.
cGAS inhibitor 36 displayed a dose-dependent reduction in cGAMP production in a ConA pharmacodynamic mouse model of acute liver injury.

Physicochemical Properties

M.Wt	421.28
Formula	C19H18Cl2N4O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-(6,7-dichloro-1-methyl-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl)(5-(2-hydroxyethoxy)pyrimidin-2-yl)methanone

References

1. Cyr P, et al. ACS Med Chem Lett. 2024 Nov 25;15(12):2201-2209.

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