diABZI STING Agonist 1 (hydrochloride)

diABZI STING agonist 1 is an activator of the stimulator of interferon genes (STING) pathway.¹ It induces secretion of IFN-β in human peripheral blood mononuclear cells (PBMCs; EC₅₀ = 130 nM). diABZI STING agonist 1 (2.5 mg/kg) increases serum levels of Ifn-β, Il-6, Tnf, and chemokine (C-X-C motif) ligand 1 (Cxcl1) in wild-type, but not Sting^-/-, mice. It inhibits the cytopathic effect of the common cold human coronavirus 229E (HCoV-229E) in infected MRC-5 cells (EC₅₀ = 3 nM). diABZI STING agonist 1 also decreases the level of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RNA in primary human bronchial airway epithelial cells in an air-liquid interface assay.² It decreases tumor volume and increases survival in a CT26 murine colorectal cancer model when administered at a dose of 3 mg/kg. This compound is expected to exist in one or both tautomeric forms.³

WARNING This product is not for human or veterinary use.

1. Ramanjulu, J.M., Pesiridis, G.S., Yang, J., et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature 564(7736), 439-443 (2018).

2. Zhu, Q., Zhang, Y., Wang, L., et al. Inhibition of coronavirus infection by a synthetic STING agonist in primary human airway system. Antiviral Res. 187, 105015 (2021).

3. Song, Z., Wang, X., Zhang, Y., et al. Structure-activity relationship study of amidobenzimidazole analogues leading to potent and systemically administrable stimulator of interferon gene (STING) agonists. J. Med. Chem. 64(3), 1649-1669 (2021).