CAY10678

CAY10678 is a selective small molecule inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), a key enzyme in the conversion of PGH2 to the pro-inflammatory mediator prostaglandin E2 (PGE2). It inhibits human and rat mPGES-1 with IC50 values of 0.09 µM and 0.9 µM, respectively, showing minimal effects on COX-1, COX-2, prostacyclin synthase (PGIS), and hematopoietic prostaglandin D synthase (PGDS) at relevant concentrations. It reduces lipocalin-type PGDS activity by about 60% at 50 µM. CAY10678 dose-dependently inhibits PGE2 synthesis and cell recruitment in models of inflammation and demonstrates anti-tumor effects in mouse models, delaying tumor growth and lowering PGE2 levels in tumor tissue. Its main research application is as a tool compound for studying inflammation, cancer, and immuno-oncology[1][3][5][7].

Other names

CAY10678CAY-10678CAY 10678mPGES-1 Inhibitor IIImPGES1 Inhibitor IIImPGES 1 Inhibitor IIIC3C-3C 3N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide