PGK1-IN-1 (Compound 6e) is a potent and selective PGK1 inhibitor ( IC50: 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) -induced experimental colitis in mice. PGK1-IN-1 can be used for research of inflammatory bowel disease (IBD) [1].
References:
[1]. Huang Z, et al. Discovery of Novel Purine Derivatives as Potent and Orally Bioavailable PGK1 Inhibitors for the Treatment of Inflammatory Bowel Disease. J Med Chem. 2025 Oct 23;68(20):21394-21411.
References:
[1]. Huang Z, et al. Discovery of Novel Purine Derivatives as Potent and Orally Bioavailable PGK1 Inhibitors for the Treatment of Inflammatory Bowel Disease. J Med Chem. 2025 Oct 23;68(20):21394-21411.