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-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-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-180795
    PKM2 activator 11
    		Activator
    PKM2 activator 11 (Compound 23) is a PKM2 activator with an AC50 value of 92.12 nM. PKM2 activator 11 promotes PKM2 tetramerization and inhibits its nuclear translocation. PKM2 activator 11 suppresses glycolysis and the PKM2/STAT3 signaling pathway. PKM2 activator 11 induces Apoptosis. PKM2 activator 11 exhibits anti-CRC activity in vitro with potency and selectivity.
    PKM2 activator 11
  • 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-111936
    ML 083
    		Activator
    ML083 is a member of a series of highly specific allosteric activators for the tumor-specific isoform of human pyruvate kinase (M2 isoform). ML083 affects the cooperativity of phosphoenolpyruvate (PEP) binding. ML083 can be used in the research of tumors.
    ML 083
  • 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-180796
    PKM2 agonist-1
    		Agonist
    PKM2 agonist-1 (Compound D16) is a highly effective, allosteric PKM2 agonist with an AC50 value of 77 nM. PKM2 agonist-1 inhibits Ang II-induced smooth muscle cell phenotypic switching. PKM2 agonist-1 effectively prevents aortic dissection and results in reduced mortality.
    PKM2 agonist-1
  • 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)
  • 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-103617R
    PKM2-IN-1 (Standard)
    		Inhibitor
    PKM2-IN-1 (Standard) is the analytical standard of PKM2-IN-1 (HY-103617). This product is intended for research and analytical applications. PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
    PKM2-IN-1 (Standard)
  • HY-N3011R
    Iridin (Standard)
    		Inhibitor
    Iridin (Standard) is the analytical standard of Iridin. This product is intended for research and analytical applications. Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.
    Iridin (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity