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Description: RU.521 (RU3205217) is a selective cyclic GMP-AMP synthetase (cGAS) inhibitor (mouse: IC50=0.11 µM), (human: IC50=2.94 µM). RU.521 is an inhibitor of the receptor activated by dsDNA (IC50=700 nM). RU.521 inhibits cGAS-mediated interferon upregulation. RU.521 reduces constitutive interferon expression in macrophages derived from a mouse model of Aicardi-Goutieres syndrome. Target: DNA, cGAS. Smiles: Cc1nn(c(O)c1C1OC(=O)c2ccccc12)-c1nc2ccc(Cl)c(Cl)c2[nH]1. References: Tan J, et al. Synthesis and Pharmacological Evaluation of Tetrahydro-gamma-carboline Derivatives as Potent Anti-inflammatory Agents Targeting Cyclic GMP-AMP Synthase. J Med Chem. 2021 Jun 10,64(11):7667-7690.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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