KH176m is the major active metabolite of KH176 ( HY-121577 ). KH176m is a microsomal prostaglandin E synthase-1 ( mPGES-1 ) inhibitor that can cross the blood-brain barrier, with an IC 50 of 0.16 µM against mouse mPGES-1 and 1.51 µM against human mPGES-1. KH176m blocks LPS- or IL-1β-induced PGE 2 production, scavenges ROS , inhibits lipid peroxidation, accelerates NADPH consumption, suppresses the growth of prostate cancer spheroids, reduces the CD44 + CD24 − prostate cancer stem cell population, and protects fibroblasts with oxidative phosphorylation defects from redox stress-induced death. KH176m can be used in research related to mitochondrial diseases, inflammatory pain, inflammatory neurological diseases, inflammatory cancers, and prostate cancer .
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