Description
Microsomal Prostaglandin E
2 Synthase-
1 (mPGES-
1), with cyclooxygenase-
2 (COX-
2), synthesizes PGE
2, 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 (IC
50 = 1.3 μM) and 5-
LO (IC
50 = 1.0 μM). It effectively inhibits PGE
2 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.
