Literature summary for 2.7.1.40 extracted from

Vander Heiden, M.G.; Christofk, H.R.; Schuman, E.; Subtelny, A.O.; Sharfi, H.; Harlow, E.E.; Xian, J.; Cantley, L.C.
Identification of small molecule inhibitors of pyruvate kinase M2 (2010), Biochem. Pharmacol., 79, 1118-1124.

Search for more literature for 2.7.1.40

Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Escherichia coli	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
(2'E)-2,2'-(1E,3E)-prop-1-en-1-yl-3-ylidenebis(1-butyl-5,6-dichloro-3-pentyl-2,3-dihydro-1H-benzimidazole)	86% inhibition at 0.03 mM	Homo sapiens
5-(2,5-dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid	81% inhibition at 0.03 mM	Homo sapiens
[(5Z)-5-(4-[[(2-iodophenyl)carbonyl]oxy]benzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid	84% inhibition at 0.03 mM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
Ni-agarose bead chromatography	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
HCC-827 cell	-	Homo sapiens	-
additional information	cancer cells universally express the M2 isoform of pyruvate kinase	Homo sapiens	-
NCI-H1299 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor	Comment	Organism	Structure
ADP	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.01	-	in 50 mM Tris, pH 7.5, at 22°C	Homo sapiens	5-(2,5-dimethyl-1H-pyrrol-1-yl)-2-hydroxybenzoic acid
0.02	-	in 50 mM Tris, pH 7.5, at 22°C	Homo sapiens	[(5Z)-5-(4-[[(2-iodophenyl)carbonyl]oxy]benzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid

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Release 2023.1 (January 2023)