| Bioactivity | RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS)[1]. | ||||||||||||
| Target | IC50: 0.7 μM (dsDNA) | ||||||||||||
| Invitro | RU.521 (0.1 nM-1000 μM; 72 h) suppresses dsDNA-induced signaling in macrophage cells[1].RU.521(0-100 μM; 24 h) selectively inhibits cGAS-mediated signaling[1]. | ||||||||||||
| In Vivo | RU.521 (5 mg/kg ; i.p. once) reduces symptoms from sepsis in mice[2]. Animal Model: | ||||||||||||
| Name | RU.521 | ||||||||||||
| CAS | 2262452-06-0 | ||||||||||||
| Formula | C19H12Cl2N4O3 | ||||||||||||
| Molar Mass | 415.23 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Vincent J, et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. [2]. Xu Q, et al. Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice. Life Sci. 2020 Nov 1;260:118315. |