RGNCY-0080 (RU.521 cGAS inhibitor)

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RU.521 is a potent and selective inhibitor of cGAS (GMP-AMP synthase) dsDNA-dependent enzymatic activity in vitro and in cells including primary macrophages taken from a Trex1 null mouse model of Aicardi-Goutieres Syndrome autoimmunity. Furthermore, the inhibition of cGAS signalling by RU.521 results in the reduction of constitutive interferon expression in the macrophages from Trex1 null mice.  RU.521 is a useful tool in the understanding of cGAS and can serve as a molecular scaffold for development of autoimmune therapies.  IC50=0.7μM inhibition of cGAS-dependent interferon induction in dsDNA-stimulated RAW macrophages. 

Systematic Name: 3-(1-(6,7-dichloro-1H-benzo[d]imidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl)isobenzofuran-1(3H)-one

SMILES: ClC1=CC=C2C(NC(N3N=C(C)C(C4C(C=CC=C5)=C5C(O4)=O)=C3O)=N2)=C1Cl

Formula: C19H12Cl2N4O3

Mol Wt:   415.23

PMID: 28963528

Tags: small molecule, autoimmune, cGAS, interferon, GMP-AMP synthase, macrophage, Trex1, RGNCY-0080