STING agonist-4

STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant ( IC 50 ) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole ( ABZI )-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function In Vitro STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC 50 of 3.1 μM. STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (K d ) of approximately 1.6 nM. STING agonist-4 (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC 50 of 53.9 μM. STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human peripheral blood mononuclear cells (PBMCs) Concentration: 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM Incubation Time: 2 hours Result: Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β. Form:Solid IC50& Target:IC50: 20 nM (STING agonist-4)

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