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].

Product Specifications

CAS Number

[3093312-81-0]

UNSPSC

12352005

Target

Phosphoglycerate Kinase (PGK)

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

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

Molecular Formula

C22H28N6O3

Molecular Weight

424.50

References & Citations

[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.