产品描述:
RU-521 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50 = 0.11 µM).{57434} It inhibits dsDNA-, but not IFN-β- or 5'ppp-HP20 RNA-, induced IFN-β1-dependent gene expression in reporter assays and does not inhibit Pam3CSK4-, poly(I:C)-, or LPS-induced Il6 mRNA expression in RAW 264.7 cells, indicating selectivity for cGAS-mediated signaling. It reduces basal Ifnb1 mRNA expression in bone marrow-derived macrophages (BMDMs) generated from the Trex1-/- mouse model of Aicardi-Goutières syndrome, an autoimmune disorder characterized by constitutive activation of cGAS and IFN overproduction.