Microsomal Prostaglandin E₂ Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE₂, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC₅₀ = 1.3 μM) and 5-LO (IC₅₀ = 1.0 μM).¹ It effectively inhibits PGE₂ and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.¹

1 Koeberle, A., Zettl, H., Greiner, C., et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E₂ synthase-1 and 5-lipoxygenase. J Med Chem 51 8068-8076 (2008).

Koeberle, A., Zettl, H., Greiner, C., et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E₂ synthase-1 and 5-lipoxygenase. J Med Chem 51 8068-8076 (2008).

CAY10589 is available in the following screening library:

• Bio-active Lipid I Screening Library (96-Well)