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

Pyruvate Kinase

Pyruvate Kinase

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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 Chemical Structure
  • 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.
    Shikonin
  • 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.
    TEPP-46
  • 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.
    PKM2-IN-1
  • 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.
    DASA-58
  • HY-12689
    Mitapivat
    		Activator 99.83%
    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.
    Mitapivat
  • HY-156375
    PKM2 activator 6
    		Activator
    PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM).
    PKM2 activator 6
  • HY-157913
    PKM2-IN-6
    		Inhibitor
    PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.
    PKM2-IN-6
  • HY-161337
    PKL-IN-1
    		Inhibitor
    PKL-IN-1 (Compound 12a) is a potent pyruvate kinase L (PKL) inhibitor with IC50 values of 0.07 μM and 0.18 μM for PKL and PKR subtypes, respectively. PKL-IN-1 can inhibit 96.6% PKL activity at 10 μM concentration.
    PKL-IN-1
  • HY-139573
    Etavopivat
    		Activator 98.70%
    Etavopivat is a potent, selective, and orally active erythrocyte pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects that can be used in studies of sickle cell disease and other haemoglobinopathies.
    Etavopivat
  • HY-147368
    PKM2 activator 2
    		Activator 99.48%
    PKM2 activator 2 (compound 28) is a pyruvate kinase M2 (PKM2) activitor with an AC50 value of 66 nM. PKM2 activator 2 can restore normal glycolytic metabolism in cells.
    PKM2 activator 2
  • 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.
    PKR activator 3
  • HY-D1456
    TEPC466
    		99.43%
    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.
    TEPC466
  • HY-135884
    Tebapivat
    		Activator 99.66%
    Tebapivat (PKR activator 2) is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.
    Tebapivat
  • HY-135883
    PKR activator 1
    		Activator
    PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.
    PKR activator 1
  • 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.
    PKM2 activator 5
  • 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.
    ML202
  • 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.
    (Rac)-Etavopivat
  • 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.
    CIAC001
  • 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.
    PKM2 activator 4
  • HY-148615
    NPD10084
    		Inhibitor
    NPD10084 is a pyruvate kinase PKM2 inhibitor that inhibits non-glycolytic signaling in cancer cells. NPD10084 disrupts the interaction between PKM2 and β-catenin or STAT3 and inhibits downstream signaling. NPD10084 has antiproliferative activity against colorectal cancer cells in vitro and in vivo.
    NPD10084
Cat. No. Product Name / Synonyms Application Reactivity