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-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-155850
    CIAC001
    		Inhibitor 99.70%
    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-P2806A
    Pyruvate Kinase (PK),Rabbit Muscle
    Pyruvate Kinase (PK),Rabbit Muscle (ATP:Pyruvate 2-0-phosphotransferase,PK) is a biological material or organic compound that can be used in life science research.
    Pyruvate Kinase (PK),Rabbit Muscle
  • HY-148615
    NPD10084
    		Inhibitor 99.69%
    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
  • HY-N7064
    Iminostilbene
    		Inhibitor 99.34%
    Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
    Iminostilbene
  • 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-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-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-159095
    PKR activator 5
    		Activator
    PKR activator 5 (Compound 18) is an activator for pyruvate kinase R (PKR) with an AC50 of 28 nM.
    PKR activator 5
  • HY-155216
    PKM2 activator 10
    		Activator
    PKM2 activator 10 (Compd I) is a PKM2 activator with anti-tumor activity. PKM2 activator 10 can be utilized in cancer research.
    PKM2 activator 10
  • HY-132215
    PF-06284674
    		Activator
    PF-06284674 (PKM2 activator 1) (Compound 8) is a PKM2 activator that can be used in cancer research.
    PF-06284674
  • HY-B0404AR
    Benserazide hydrochloride (Standard)
    		Inhibitor
    Benserazide hydrochloride (Standard) (Serazide (Standard)) is the analytical standard of Benserazide hydrochloride (HY-B0404A). This product is intended for research and analytical applications. Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma.
    Benserazide hydrochloride (Standard)
  • HY-168883
    PKM2 modulator 2
    		Inhibitor
    PKM2 modulator 2 (compound C599) is a potent PKM2 inhibitor. PKM2 modulator 2 shows antiproliferative activity. PKM2 modulator 2 induces apoptosis. PKM2 modulator 2 has the potential for the research of glioblastoma.
    PKM2 modulator 2
  • HY-170577
    PKM2-IN-8
    		Inhibitor
    PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC50 = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma.
    PKM2-IN-8
  • 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-121275
    Benserazide
    		Inhibitor
    Benserazide is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide is also a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the study of Parkinson's disease and melanoma.
    Benserazide
  • HY-N7064R
    Iminostilbene (Standard)
    		Inhibitor
    Iminostilbene (Standard) is the analytical standard of Iminostilbene. This product is intended for research and analytical applications. Iminostilbene is a a chemical precursor of carbamazepine.
    Iminostilbene (Standard)
  • HY-168337
    SET-171
    		Inhibitor
    SET-171 is a JNK (c-Jun N-terminal kinase) inhibitor that exhibits significant anticancer activity and lipid metabolism regulation by inhibiting liver pyruvate kinase (PKL) expression. In anticancer studies, SET-171 shows IC50 values of 8.82 μM and 2.97 μM against HepG2 and Huh7 cell lines, respectively, indicating high cytotoxicity. Additionally, in non-alcoholic fatty liver disease (NAFLD)-related studies, SET-171 significantly reduces triacylglycerol (TAG) levels and inhibits the expression of steatosis-related proteins. SET-171 holds promise for research on hepatocellular carcinoma (HCC) and NAFLD.
    SET-171
  • HY-12689B
    Mitapivat hemisulfate
    		Activator
    Mitapivat hemisulfate is an orally active pyruvate kinase allosteric activator. Mitapivat hemisulfate 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 hemisulfate can be used in study of PK deficiency.
    Mitapivat hemisulfate
Cat. No. Product Name / Synonyms Application Reactivity