1H-Benzimidazole-5-carboxamide, 1-[4-[5-(aminocarbonyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-1H-benzimidazol-1-yl]butyl]-N-(2-aminoethyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-

Biological Activity

diABZI-C2-NH2, an active analogue containing a primary amine functionality, is a STING agonist[1]. The author developed a linking strategy to synergize the effect of two symmetry-related amidobenzimidazole (ABZI)-based compounds to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function. Intravenous administration of a diABZI STING agonist to immunocompetent mice with established syngeneic colon tumours elicited strong anti-tumour activity, with complete and lasting regression of tumors[1]. diABZI-C2-NH2 is covalently immobilized on sepharose beads and is used to affinity-capture potential target proteins from a THP1 cell lysate[1].

References

[1]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity [published correction appears in Nature. 2019 Jun;570(7761):E53]. Nature. 2018;564(7736):439-443.