1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Pyruvate Kinase

Pyruvate Kinase

Pyruvate kinase is an enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP in glycolysis and plays a role in regulating cell metabolism. There are four mammalian pyruvate kinase isoforms with unique tissue expression patterns and regulatory properties. Pyruvate kinase has four different tissue-specific isozymes in animals, PKL, PKR, PKM1, and PKM2. The L and R isozymes are expressed in the liver (L) and red blood cells (R), whereas PKM2 is expressed in early embryonic cells and other proliferating cells, and PKM1 is expressed in the brain, skeletal muscle, and heart which need high energy.

PKM1 and PKM2 are formed by a single mRNA transcript of the PKM gene by alternative splicing. The oligomers of PKM2 exist in high activity tetramer and low activity dimer forms. The dimer PKM2 regulates the rate-limiting step of glycolysis that shifts the glucose metabolism from the normal respiratory chain to lactate production in tumor cells. Besides its role as a metabolic regulator, it also acts as a protein kinase, which contributes to tumorigenesis. PKM2 serves as a promising target for cancer treatment.

Pyruvate Kinase Related Products (10):

Cat. No. Product Name Effect Purity
  • HY-18657
    Activator 99.71%
    TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR.
  • HY-N0822
    Inhibitor 99.80%
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
  • HY-103617
    Inhibitor 99.61%
    PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
  • HY-19330
    Activator 99.65%
    DASA-58 is a potent activator of pyruvate kinase M2 (PKM2) with an AC90 of 680 nM, and an AC50 of 38 nM.
  • HY-12689
    Activator 99.85%
    Mitapivat (AG-348) is a potent, orally active, and allosteric activator of pyruvate kinase with an AC50 of 20 nM. Mitapivat (AG-348) increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes. Mitapivat (AG-348) has the potential for restoring the glycolytic pathway activity with PK deficiency.
  • HY-19702
    Activator 99.14%
    PKR-IN-2 is a pyruvate kinase isoform PKR activator extracted from patent WO2014139144A1, compound 160. PKR-IN-2 can be used for the research of PKR function related diseases, including cancer, diabetes, obesity, autoimmune disorders, and benign prostatic hyperplasia.
  • HY-135884
    PKR activator 2
    PKR activator 2 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.
  • HY-139573
    Etavopivat is a potent, selective, orally bioavailable red blood cell (RBC) pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects.
  • HY-135883
    PKR activator 1
    PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.
  • HY-139667
    PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
Isoform Specific Products

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