YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 ( mPGES-1 ; IC 50 = 3.4 μM) and 5-lipoxygenase ( 5-LOX ; IC 50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 ( K D = 10-14 μM). YS121 dose-dependently reduces PGE 2 production with an EC 50 of 12 μM in IL-1β-stimulated A549 cells. YS121 (compound 9) activates PPAR -α and -γ ( EC 50 = 1 and 3.6 μM, respectively). YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research.
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