C53

C53 is a STING agonist.¹ It activates human wild-type STING (EC₅₀ = 185 nM), as well as STING containing the polymorphisms R232, H232, or HAQ in HEK293 cells in an interferon-stimulated gene 54 (ISG54) luciferase reporter assay when used at a concentration of 10 µM. C53 (10 µM) induces the expression of IFN-α, IFN-β, TNF-α, chemokine (C-X-C motif) ligand 10 (CXCL10), IL-12p40, and IL-6 in isolated human monocyte-derived dendritic cells (hMO-DCs). It also increases the expression of the dendritic cell markers CD83 and CD86 in hMO-DCs when used at a concentration of 10 µM.

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1. Pryde, D.C., Middya, S., Banerjee, M., et al. The discovery of potent small molecule activators of human STING. Eur. J. Med. Chem. 209, 112869 (2021).