MF63

MF63 is a potent, selective, and orally active small molecule inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). Developed by Merck Frosst, it specifically blocks the terminal enzyme responsible for the conversion of prostaglandin H2 (PGH2) into prostaglandin E2 (PGE2). Unlike non-selective NSAIDs or COX-2 inhibitors, MF63 reduces PGE2 production without suppressing other prostanoids like prostacyclin (PGI2) or thromboxane A2 (TXA2), which is intended to avoid the cardiovascular risks associated with systemic COX inhibition. In preclinical research, MF63 has demonstrated the ability to reduce PGE2 levels, inhibit tumor cell proliferation, and induce apoptosis in various cancer models, including bladder cancer. It is also frequently utilized as a tool compound in studies investigating inflammation and pain.

Other names

2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)isophthalonitrile