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Synonyms: compound 1 [PMID: 21958545] | DASA58 | ML-203 | ML203
Compound class: Synthetic organic
Comment: DASA-58 is an activator of tumour-associated pyruvate kinase M2 (PKM2) . PKM2 activation has potential to interfere with the anabolic metabolic pathway that is utilised by cancer cells to maintain high levels of proliferation. Like TEPP-46, DASA-58 promotes formation of highly active PKM2 tetramers and suppresses tumour expansion in vivo .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A et al.. (2012)
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Nat Chem Biol, 8 (10): 839-47. [PMID:22922757]
2. Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M et al.. (2011)
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Bioorg Med Chem Lett, 21 (21): 6322-7. [PMID:21958545]