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Literature summary for 2.7.1.40 extracted from

  • Boxer, M.B.; Jiang, J.K.; Vander Heiden, M.G.; Shen, M.; Skoumbourdis, A.P.; Southall, N.; Veith, H.; Leister, W.; Austin, C.P.; Park, H.W.; Inglese, J.; Cantley, L.C.; Auld, D.S.; Thomas, C.J.
    Evaluation of substituted N,N’-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase (2009), J. Med. Chem., 53, 1048-1055.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
(2R)-1-[(2,6-difluorophenyl)sulfonyl]-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
 Homo sapiens
(2R)-4-[(2,6-difluorophenyl)sulfonyl]-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
 Homo sapiens
(2S)-1-[(2,6-difluorophenyl)sulfonyl]-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
 Homo sapiens
(2S)-4-[(2,6-difluorophenyl)sulfonyl]-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
-
 Homo sapiens
1-[(2,6-difluorophenyl)sulfonyl]-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-2-one
-
 Homo sapiens
3-([4-[(2,6-difluoro-4-methoxyphenyl)sulfonyl]-1,4-diazepan-1-yl]sulfonyl)aniline
-
 Homo sapiens
3-([4-[(2,6-difluoro-4-methoxyphenyl)sulfonyl]piperazin-1-yl]sulfonyl)aniline highly potent activator of PKM2 Homo sapiens
3-([4-[(2,6-difluorophenyl)sulfonyl]piperazin-1-yl]sulfonyl)aniline highly potent activator of PKM2 Homo sapiens
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]aniline highly potent activator of PKM2 Homo sapiens
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-1-yl]sulfonyl]aniline highly potent activator of PKM2 Homo sapiens
4-[(2,6-difluorophenyl)sulfonyl]-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-2-one
-
 Homo sapiens
6-([4-[(2,6-difluorophenyl)sulfonyl]cyclohexyl]sulfonyl)-2,3-dihydro-1,4-benzodioxine
-
 Homo sapiens
N-[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperidin-4-yl]-2,6-difluorobenzenesulfonamide
-
 Homo sapiens
N-[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)pyrrolidin-3-yl]-2,6-difluorobenzenesulfonamide
-
 Homo sapiens
N-[1-[(2,6-difluorophenyl)sulfonyl]azetidin-3-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
 Homo sapiens
N-[1-[(2,6-difluorophenyl)sulfonyl]piperidin-4-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
 Homo sapiens
N-[1-[(2,6-difluorophenyl)sulfonyl]pyrrolidin-3-yl]-2,3-dihydro-1,4-benzodioxine-6-sulfonamide
-
 Homo sapiens
N-[[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)azetidin-3-yl]methyl]-2,6-difluorobenzenesulfonamide
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.1
-
 phosphoenolpyruvate in the presence of D-fructose 1,6-bisphosphate Homo sapiens
1.5
-
 phosphoenolpyruvate in the absence of activator Homo sapiens

Organism

Organism UniProt Comment Textmining
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
tumor cell specific pyruvate kinase isozyme M2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ADP
-
 Homo sapiens