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-12689A
    Mitapivat hemisulfate sesquihydrate
    		Activator
    Mitapivat hemisulfate sesquihydrate (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 hemisulfate sesquihydrate
  • HY-D1877
    ZY-1
    		98.91%
    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.
    ZY-1
  • 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-P3201
    PKCζ/ι pseudosubstrate inhibitor
    		Inhibitor
    PKCζ/ι pseudosubstrate inhibitor has broad-spectrum effects on the PKC enzyme family and can induce memory impairment.
    PKCζ/ι pseudosubstrate inhibitor
  • 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.
    Vitamin K5
  • 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.
    PKM2-IN-4
  • HY-169567
    PKM2-IN-9
    		Inhibitor
    PKM2-IN-9 (compound C1) is a potent inhibitor of PKM2, with the inhibition rate of 75% at 50 μM. PKM2-IN-9 plays an important role in cancer research.
    PKM2-IN-9
  • HY-B0404AS
    Benserazide-d3 hydrochloride
    		Inhibitor
    Benserazide-d3 (hydrochloride) is the deuterium labeled Benserazide hydrochloride (HY-B0404A). 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-d<sub>3</sub> hydrochloride
  • 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-168446
    PKR-IN-1
    		Inhibitor
    PKR-IN-1 (Compound 5s) is a pyruvate kinase (PK) inhibitor that has antifungal activity, with an EC50 of 0.21 μg/mL for R. solani.
    PKR-IN-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-N7108R
    7-Hydroxyflavone (Standard)
    		Inhibitor
    7-Hydroxyflavone (Standard) is the analytical standard of 7-Hydroxyflavone. This product is intended for research and analytical applications. 7-Hydroxyflavone is a flavonoid isolated from Clerodendrum phlomidis, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway. 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM. 7-Hydroxyflavone inhibits COX-2 and 5-LOX with IC50 of 27 µg/mL and 33 µg/mL. 7-Hydroxyflavone is orally active.
    7-Hydroxyflavone (Standard)
Cat. No. Product Name / Synonyms Application Reactivity