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-161519
    PKM2 activator 7
    		Activator
    PKM2 activator 7 (Compd B4) is a PKM2 activator with the AC50 of 0.144 μM. PKM2 activator 7 suppresses DSS (HY-116282C)-induced colitis by inhibiting T cell growth in mouse colitis model.
    PKM2 activator 7
  • HY-147397
    PKM2 activator 3
    		Activator
    PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer.
    (AC50: the concentration which gives 50% activation of enzyme.)
    PKM2 activator 3
  • HY-N0822R
    Shikonin (Standard)
    		Inhibitor
    Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-153354
    PKR activator 4
    		Activator
    PKR activator 4 (example 7A) is a potent pyruvate kinase R (PKR) activator. PKR activator 4 has the potential for the research of blood disorders.
    PKR activator 4
  • HY-119874
    Alkannin
    		Inhibitor
    Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent.
    Alkannin
  • HY-149275
    PKM2/PDK1-IN-1
    		Inhibitor
    PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway.
    PKM2/PDK1-IN-1
  • HY-168882
    PKM2 modulator 1
    		Inhibitor
    PKM2 modulator 1 (compound C998) is a potent PKM2 inhibitor. PKM2 modulator 1 shows antiproliferative activity. PKM2 modulator 1 induces apoptosis. PKM2 modulator 1 has the potential for the research of glioblastoma.
    PKM2 modulator 1
  • HY-W587878
    Thujopsene
    		Inhibitor
    Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation.
    Thujopsene
  • HY-N2552R
    Vitamin K5 hydrochloride (Standard)
    		Inhibitor
    Vitamin K5 (hydrochloride) (Standard) is the analytical standard of Vitamin K5 (hydrochloride). This product is intended for research and analytical applications. Vitamin K5 hydrochloride is a photosensitizer and a antimicrobial agent. Vitamin K5 hydrochloride is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 hydrochloride induces apoptosis of colon 26 cells. Vitamin K5 hydrochloride can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages[1][2][3].
    Vitamin K5 hydrochloride (Standard)
  • HY-162071
    PKM2-IN-5
    		Inhibitor
    PKM2-IN-5 (Compound G1) is an inhibitor for pyruvate kinase M2 (PKM2), with IC50 >70 μM.
    PKM2-IN-5
  • HY-169883
    PKM2-IN-7
    		Inhibitor
    PKM2-IN-7 (compound 34) can inhibit the interaction between PKM2 and ALDH1A3 without showing significant toxicity to normal cells. PKM2-IN-7 can be used for research in the field of tumors.
    PKM2-IN-7
  • HY-121275
    Benserazide
    		Inhibitor
    Benserazide is 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 research of melanoma.
    Benserazide
  • HY-12689C
    Mitapivat hydrochloride
    		Activator
    Mitapivat (AG-348) hydrochloride is an orally active and selective allosteric pyruvate kinase R (PK-R) activator. Mitapivat hydrochloride accelerates the reaction of PK-R catalyzing the conversion of phosphoenolpyruvate to pyruvate, thereby promoting the glycolytic pathway, increasing the production of adenosine triphosphate (ATP) in red blood cells, and reducing the level of 2,3-diphosphoglycerate (2,3-DPG). Mitapivat hydrochloride is promising for research of pyruvate kinase deficiency and other anemia-related diseases.
    Mitapivat hydrochloride
  • HY-165154
    Cyclamidomycin
    		Inhibitor
    Cyclamidomycin (Desdanine) is an acrylamide antibiotic with antibacterial activity. Cyclamidomycin inhibits nucleoside diphosphate kinase and pyruvate kinase (in E. coli) and oxidative phosphorylation in rat liver mitochondria. Cyclamidomycin is active against S. aureus, M. flavus, S. lutea, B. subtilis, E. coli, S. flexneri, S. typhosa, P. vulgaris, and K. pneumoniae (MICs=3.12-25 mg/ml).
    Cyclamidomycin
  • HY-134177
    2,5-Anhydro-D-glucitol-1,6-diphosphate
    		Activator
    2,5-Anhydro-D-glucitol-1,6-diphosphate is a limited stimulator of yeast Pyruvate Kinase. 2,5-Anhydro-D-glucitol-1,6-diphosphate is used as an analogue of the a-form, 2,5-anhydro-D-mannitol 1,6-bisphosphate, while is an excellent allosteric activator of Pyruvate Kinase.
    2,5-Anhydro-D-glucitol-1,6-diphosphate
  • HY-112464
    PKR Inhibitor, negative control
    		Inhibitor
    PKR Inhibitor, negative control is an inactive structural analog of RNA-dependent protein kinase (PKR) inhibitor, which can be used as a negative control. PKR Inhibitor, negative control can also inhibit LK-induced neuronal death, exhibiting significant neuroprotective effects.
    PKR Inhibitor, negative control
  • HY-N15451
    Deoxytopsentin
    		Inhibitor
    Deoxytopsentin is a compound that can be found in marine sponges. It is an inhibitor of pyruvate kinase (PK) in methicillin-resistant Staphylococcus aureus (MRSA), with an IC50 value of 240 nM. Deoxytopsentin can be used in research in the field of anti-infection .
    Deoxytopsentin
Cat. No. Product Name / Synonyms Application Reactivity