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Literature summary extracted from

  • Chen, J.; Jiang, Z.; Wang, B.; Wang, Y.; Hu, X.
    Vitamin K3 and K5 are inhibitors of tumor pyruvate kinase M2 (2012), Cancer Lett., 316, 204-210.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.40 expression of His6-tagged isozymes in Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.40 4-amino-2-methylnaphthalen-1-ol i.e. vitamin K5, shows a significantly stronger potency to inhibit isozyme PKM2 than to inhibit isozymes PKM1 and PKL Homo sapiens
2.7.1.40 menadione i.e. vitamin K3, shows a significantly stronger potency to inhibit isozyme PKM2 than to inhibit isozymes PKM1 and PKL Homo sapiens
2.7.1.40 additional information D-fructose 1,6-bisphosphate diminishes the inhibitory effects of vitamin K derivatives. No inhibition of isozyme PKM2 by vitamin K1 and vitamin K2 Homo sapiens
2.7.1.40 N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole a PKM2 inhibitor Homo sapiens
2.7.1.40 shikonin a PKM2 inhibitor Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.1.40 Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.40 ATP + pyruvate Homo sapiens
-
 ADP + phosphoenolpyruvate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.40 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.40 recombinant His6-tagged isozymes from Escherichia coli by nickel affinity chromatgraphy Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.40 HeLa cell Hela cells express PKM2 but not PKM1 or PKL Homo sapiens
-
2.7.1.40 liver isozyme PKL Homo sapiens
-
2.7.1.40 additional information isozyme PKM1 is expressed in most adult tissues Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.40 ATP + pyruvate
-
 Homo sapiens ADP + phosphoenolpyruvate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.40 PKL
-
 Homo sapiens
2.7.1.40 PKM1
-
 Homo sapiens
2.7.1.40 PKM2
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.1.40 25
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.1.40 7.5
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.40 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.40 0.028
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in absence of D-fructose 1,6-bisphosphate Homo sapiens 4-amino-2-methylnaphthalen-1-ol
2.7.1.40 0.045
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in presence of D-fructose 1,6-bisphosphate Homo sapiens 4-amino-2-methylnaphthalen-1-ol
2.7.1.40 0.0593
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in absence of D-fructose 1,6-bisphosphate Homo sapiens N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole
2.7.1.40 0.0775
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in presence of D-fructose 1,6-bisphosphate Homo sapiens N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole
2.7.1.40 0.12
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKL, in absence of D-fructose 1,6-bisphosphate Homo sapiens 4-amino-2-methylnaphthalen-1-ol
2.7.1.40 0.15
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in absence of D-fructose 1,6-bisphosphate Homo sapiens menadione
2.7.1.40 0.191
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM1, in absence of D-fructose 1,6-bisphosphate Homo sapiens 4-amino-2-methylnaphthalen-1-ol
2.7.1.40 0.381
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM2, in presence of D-fructose 1,6-bisphosphate Homo sapiens menadione
2.7.1.40 0.837
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKL, in absence of D-fructose 1,6-bisphosphate Homo sapiens menadione
2.7.1.40 3.407
-
 pH 7.5, 25°C, recombinant His6-tagged isozyme PKM1, in absence of D-fructose 1,6-bisphosphate Homo sapiens menadione

General Information

EC Number General Information Comment Organism
2.7.1.40 malfunction consequence of PKM2 inhibition is a reduced glycolytic flux, which can be reflected by the rates of cellular glucose consumption and lactate production Homo sapiens
2.7.1.40 physiological function pyruvate kinase isozyme PKM2 is a rate-limiting enzyme of aerobic glycolysis in cancer cells and plays important roles in cancer metabolism and growth. Vitamin K3/vitamin K5-enhanced toxicity of doxorubicin is associated with pyruvate kinase activity Homo sapiens