YS121

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC₅₀ = 3.4 μM) and 5-lipoxygenase (5-LOX; IC₅₀ = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (K_D = 10-14 μM)^[1]. YS121 dose-dependently reduces PGE₂ production with an EC₅₀ of 12 μM in IL-1β-stimulated A549 cells^[2]. YS121 (compound 9) activates PPAR-α and -γ (EC₅₀ = 1 and 3.6 μM, respectively)^[3]. YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research^[1]. In Vitro:YS121 (0.3-30 μM) acts as a potent and selective inhibitor of mPGES-1 in interleukin-1β-stimulated human A549 cell microsomes, concentration-dependently and non-competitively blocking the conversion of PGH₂ to PGE₂, with no marked inhibition of other PGES enzymes^[1].
YS121 (0.1-30 μM) concentration-dependently inhibits PGE₂ formation with an IC₅₀ value of 3 μM, and moderately suppresses PGE₂ synthesis in the absence of CV4151^[1].
YS121 (0.1-30 μM) inhibits PGE₂ formation without affecting the synthesis of COX-2-derived 6-keto PGF_1α and TxB₂ or COX-1-derived 12-HHT in human whole blood^[1].
YS121 (10 μM, 0-48 h) selectively modulates protein expression over a 48-hour period, specifically reducing COX-2 levels after 24 hours while leaving mPGES-1 expression unchanged^[1]. In Vivo:YS121 (1.5 mg/kg, i.p., 30 min pre-modeling, once) exhibits potent anti-inflammatory efficacy in a carrageenan-induced rat pleurisy model^[1].