PGK1-IN-1 (Compound 6e) is a potent and selective PGK1 inhibitor ( IC 50 : 33 nM). PGK1-IN-1 inhibits PGK1-mediated glycolytic metabolism and reduces glucose consumption/lactate production. PGK1-IN-1 enhances Nrf2 accumulation and HO-1 expression, and suppresses the transcription and protein levels of the inflammatory cytokines IL-1β and IL-6 . PGK1-IN-1 ameliorates Dextran sulfate sodium (DSS) ( HY-116282C )-induced experimental colitis in mice. PGK1-IN-1 can be used for research of inflammatory bowel disease (IBD).
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