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Literature summary for 2.7.1.40 extracted from

  • Adem, S.; Aslan, A.; Ahmed, I.; Krohn, K.; Guler, C.; Comakl?, V.; Demirdag, R.; Kuzu, M.
    Inhibitory and Activating Effects of Some Flavonoid Derivatives on Human Pyruvate Kinase Isoenzyme M2 (2016), Arch. Pharm., 349, 132-136.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
(1S,2S)-3-(2-hydroxy-4-methoxyphenyl)-1-(4-methoxyphenyl)propane-1,2-diol AC50 value of 0.15 mM Homo sapiens
(2R,3S)-2-phenyl-3,4-dihydro-2H-chromen-3-ol AC50 value of 0.221 mM Homo sapiens
(2R,3S)-5,7-diphenoxy-2-(3,4,5-triphenoxyphenyl)-3,4-dihydro-2H-1-benzopyran-3-ol AC50 value of 0.028 mM Homo sapiens
(3S)-7-phenoxy-2-(4-phenoxyphenyl)-3,4-dihydro-2H-1-benzopyran-3-ol AC50 value of 0.115 mM Homo sapiens
(3S,4S)-2-(3,4-diphenoxyphenyl)-5,7-diphenoxy-3,4-dihydro-2H-1-benzopyran-3,4-diol AC50 value of 0.048 mM Homo sapiens
3-(2-hydroxy-4-phenoxyphenyl)-1-(4-phenoxyphenyl)propane-1,2-diol AC50 value of 0.2 mM Homo sapiens
5-methoxy-2-[(2E)-3-(4-methoxyphenyl)prop-2-en-1-yl]phenol AC50 value of 0.027 mM Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-1-(4-methoxyphenyl)-3-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
Homo sapiens
(2R,3S)-2-(3,4-diphenoxyphenyl)-3,5,7-triphenoxy-3,4-dihydro-2H-1-benzopyran
-
Homo sapiens
3,5-diphenoxy-2-[(2E)-3-(3,4,5-triphenoxyphenyl)prop-2-en-1-yl]phenol
-
Homo sapiens
3-(2-hydroxy-4-methoxyphenyl)-1-(4-methoxyphenyl)propane-1,2-diol
-
Homo sapiens
5,7-diphenoxy-2-(3,4,5-triphenoxyphenyl)-2H-1-benzopyran
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
PKM2
-
Homo sapiens
pyruvate kinase isoenzyme M2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.045
-
at pH 8.0 and 22°C Homo sapiens 5,7-diphenoxy-2-(3,4,5-triphenoxyphenyl)-2H-1-benzopyran
0.058
-
at pH 8.0 and 22°C Homo sapiens (2R,3S)-2-(3,4-diphenoxyphenyl)-3,5,7-triphenoxy-3,4-dihydro-2H-1-benzopyran
0.145
-
at pH 8.0 and 22°C Homo sapiens 3,5-diphenoxy-2-[(2E)-3-(3,4,5-triphenoxyphenyl)prop-2-en-1-yl]phenol
0.163
-
at pH 8.0 and 22°C Homo sapiens (2E)-1-(4-methoxyphenyl)-3-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
0.295
-
at pH 8.0 and 22°C Homo sapiens 3-(2-hydroxy-4-methoxyphenyl)-1-(4-methoxyphenyl)propane-1,2-diol

General Information

General Information Comment Organism
metabolism pyruvate kinase isoenzyme M2 plays an important role in the control of glucose metabolism Homo sapiens