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STING agonist D61 (D61) is an agonist of stimulator of interferon genes (STING).1 It induces expression of an IFN3-inducible secreted alkaline phosphatase (SEAP) reporter gene and an IFN-β-inducible reporter gene in cell-based assays (EC50s = 52.9 and 116 nM, respectively). D61 (4, 6, and 8 µM) increases the expression of mRNA encoding IFN-β and chemokine (C-X-C motif) ligand 10 (CXCL10) and phosphorylation of TANK-binding kinase 1 (TBK1), IRF3, and STING in THP-1 monocytes. In vivo, D61 (0.25 mg/kg every other day) reduces tumor volume without affecting body weight in a CT26 murine colon cancer model.
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1. Development of orally bioavailable amidobenzimidazole analogues targeting stimulator of interferon gene (STING) receptor. J. Med. Chem. 66(8), 5584-5610 (2023).