1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Kinase (PGK)

Phosphoglycerate Kinase (PGK)

Phosphoglycerate Kinase

Phosphoglycerate Kinase (PGK) is a key enzyme involved in glycolysis and gluconeogenesis. Currently, there are two isoenzymes of Phosphoglycerate Kinase, PGK1 and PGK2. Phosphoglycerate Kinase (PGK) catalyzes the reversible transfer of a phosphate group from 1,3-bisphosphoglycerate to ADP, producing 3-phosphoglycerate and ATP. This reaction is the first step in ATP production during glycolysis. Abnormal function of Phosphoglycerate Kinase (PGK) can disrupt cellular energy metabolism, thereby triggering and influencing the occurrence and development of various diseases, such as cancer, hemolytic anemia, neuromuscular dysfunction, etc[1].

Phosphoglycerate Kinase (PGK) Isoform Specific Products:

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W195984
    Z57346765
    99.85%
    Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer.
    Z57346765
  • HY-178761
    PGK1-IN-1
    Inhibitor 99.78%
    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).
    PGK1-IN-1
  • HY-N8540
    Ilicicolin H
    Inhibitor
    Ilicicolin H is a selective and non-ATP-competitive phosphoglycerate kinase 1 (PGK1) (IC50 = 9.02 μM) and mitochondrial cytochrome bc1 reductase (IC50 = 2-3 ng/mL) inhibitor. Ilicicolin H directly binds to PGK1 with KD of 60 μM .Ilicicolin H can inhibit cell proliferation and induce apoptosis. Ilicicolin H can inhibit the lactate production and glucose uptake of hepatocellular carcinoma (HCC) cells. Ilicicolin H has a broad antifungal spectrum including C. albicans, Cryptococcus and A. fumigatus. Ilicicolin H can be used for the researches of cancer and infection, such as hepatocellular carcinoma (HCC) and C. albicans infection.
    Ilicicolin H
  • HY-178989
    PGK1-IN-2
    Inhibitor
    PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma.
    PGK1-IN-2
  • HY-177944
    DC-PGKI
    Inhibitor
    DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC50 = 0.16 Μm, Kd = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis.
    DC-PGKI

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