Pyruvate Kinase

Pyruvate kinase activators and inhibitors act on the enzyme that catalyzes the final step of glycolysis. Pyruvate kinase transfers phosphate from phosphoenolpyruvate to adenosine diphosphate (ADP), producing pyruvate and adenosine triphosphate (ATP). The M2 isoform (PKM2), expressed in proliferating cells, switches between active tetramers and less active dimers. In 2008 PKM2 was shown to support aerobic glycolysis and tumor growth in xenografts. TEPP-46 and DASA-58 activate PKM2 by promoting tetramer formation, as reported in 2012. Mitapivat is an activator of pyruvate kinase isoforms, including the red blood cell enzyme. Shikonin, listed as (Rac)-Shikonin, and PKM2-IN-1 inhibit PKM2 in studies of cancer cell glycolysis. Several other entries have no direct link to pyruvate kinase.

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  • IS20
    Cat. No.
    A25737

    IS20

    IS20 is a selective Prokineticin receptor 1 (PKR1) agonist that activates the Akt and MAPK signaling pathways. This compound has demonstrated the ability to reduce Doxorubicin-induced apoptosis and reactive oxygen species (ROS) production, thereby offering cardioprotective effects against Doxorubicin-induced toxicity. In preclinical mouse models, IS20 has been shown to enhance survival rates and improve cardiac function without affecting the cytotoxicity or antitumor efficacy of Doxorubicin in breast cancer cells. This makes IS20 a valuable reagent for cancer research, particularly in studies addressing the side effects of chemotherapy on cardiac health.

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