PGK1-IN-1 

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) (HY-116282C)-induced experimental colitis in mice. PGK1-IN-1 can be used for research of inflammatory bowel disease (IBD)^[1].

424.50

C₂₂H₂₈N₆O₃

3093312-81-0

Solid

White to off-white

COC1=CC(NC(N=C(N[C@H]2CC[C@@H](CC2)O)N=C34)=C4N=CN3C5CC5)=CC(OC)=C1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]