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.

Cat. No. Product Name Effect Purity
  • HY-N0822
    Shikonin
    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-18657
    TEPP-46
    Activator 99.65%
    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-16214
    FX-11
    Activator 98.44%
    FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) specific inhibitor, with a Ki of 8 μM. FX-11 can effectively activate PKM2 (pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.
  • HY-103617
    PKM2-IN-1
    Inhibitor 99.61%
    PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
  • HY-19330
    DASA-58
    Activator 99.67%
    DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer.
  • HY-155850
    CIAC001
    Inhibitor
    CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction.
  • HY-D1877
    ZY-1
    ZY-1 is a control molecule of ZY-2 (HY-D1876, a PKM2 fluorescent probe). ZY-1 shows a low fluorescence emission in HeLa, a cervical cancer cell abundant in PKM2 expression.
  • HY-155849
    PKM2-IN-4
    Inhibitor
    Pkm2-in-4 (compound 5C) is a selective inhibitor of PKM2 (IC50=0.35 μM), which regulates pyruvate-dependent respiration and induces mitochondrial H202 production rate and electron transport system coupling.
  • HY-12689
    Mitapivat
    Activator 99.85%
    Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.
  • HY-19702
    PKR activator 3
    Activator 99.87%
    PKR activator 3 is a pyruvate kinase isoform PKR activator extracted from patent WO2014139144A1, compound 160. PKR activator 3 can be used for the research of PKR function related diseases, including cancer, diabetes, obesity, autoimmune disorders, and benign prostatic hyperplasia.
  • HY-139573
    Etavopivat
    Activator 98.70%
    Etavopivat is a potent, selective, orally bioavailable red blood cell (RBC) pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects.
  • HY-147368
    PKM2 activator 2
    Activator 99.48%
    PKM2 activator 2 is a pyruvate kinase M2 (PKM2) activitor with an AC50 value of 66 nM. PKM2 activator 2 may show anti-tumor proliferation effect and relieve the Warburg effect, while PKM2 activation can restore normal glycolytic metabolism in cells.
  • HY-D1456
    TEPC466
    TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe. TEPC466 shows a high degree of selectivity and sensitivity for the detection of PKM2 protein via the AIE effect. EPC466 can be used for the detection of PKM2. TEPC466 is successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. TEPC466 is a useful tool for cancer diagnosis and research.
  • HY-135884
    Tebapivat
    Activator 99.66%
    Tebapivat (PKR activator 2) is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.
  • HY-135883
    PKR activator 1
    Activator
    PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.
  • HY-139573A
    (Rac)-Etavopivat
    Activator 99.87%
    (Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat (HY-139573). Etavopivat is an orally active erythrocyte pyruvate kinase-R (PKR) activator that can be used in studies of sickle cell disease and other haemoglobinopathies.
  • HY-148313
    PKM2 activator 4
    Activator
    PKM2 activator 4 is a PKM2 activator with an AC50 value of 1-10 μM. PKM2 activator 4 can be used for the research of cancer.
  • HY-148324
    PKM2 activator 5
    Activator
    PKM2 activator 5 (compound 8) is a PKM2 activator with an AC50 value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells.
  • HY-110124
    ML202
    Activator 99.27%
    ML202 is a highly specific allosteric activator of human pyruvate kinase M2 (hPK-M2), which can affect the cooperativity of phosphoenolpyruvate (PEP) binding, while adenosine diphosphate (ADP) binding almost no effect.
  • HY-B1814
    Vitamin K5
    Inhibitor
    Vitamin K5 (Synkamin) is a photosensitizer and a antimicrobial agent. Vitamin K5 is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 induces apoptosis of colon 26 cells. Vitamin K5 can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages.
Cat. No. Product Name / Synonyms Application Reactivity