Prostaglandin E₂ Inhibitor 3

Prostaglandin E₂ (PGE₂) inhibitor 3 is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC₅₀ = 0.2 µM).¹ It is selective for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in cell-free assays at 10 µM. PGE₂ inhibitor 3 inhibits IL-1β-induced production of PGE₂ (Item No. 14010) in A549 cells and LPS-induced IL-6 and PGE₂ production in J774A.1 macrophages when used at concentrations of 10 and 1 µM, respectively. It also inhibits the formation of 5-LO products, including leukotriene B₄ (LTB₄; Item No. 20110) and 5-H(p)ETE, induced by the calcium ionophore A23187 (Item Nos. 11016 | 22030) alone or with arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) and A23187 (IC₅₀s = 4.9 and 5.2 µM, respectively). In vivo, PGE₂ inhibitor 3 (10 mg/kg) prevents leukocyte infiltration into the peritoneal fluid in a mouse model of zymosan-induced peritonitis.

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1. Potenza, M., Giodano, A., Chini, M.G., et al. Identification of 2-aminoacyl-1,3,4-thiadiazoles as prostaglandin E₂ and leukotriene biosynthesis inhibitors. ACS Med. Chem. Lett. 14(1), 26-34 (2023).