Synonyms: compound 46 [PMID: 20451379] | ML-265 | ML265 | TEPP46
Compound class:
Synthetic organic
Comment: TEPP-46 is an activator of tumour-associated pyruvate kinase M2 (PKM2) [1,4-5]. It promotes formation of the highly active PKM2 tetramer, and reduces cancer cell proliferation by interfering with anabolic metabolism. It is active in a mouse xenograft model [4].
Ligand Activity Visualisation ChartsThese 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. ✖ |
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References |
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. Angiari S, Runtsch MC, Sutton CE, Palsson-McDermott EM, Kelly B, Rana N, Kane H, Papadopoulou G, Pearce EL, Mills KHG et al.. (2020)
Pharmacological Activation of Pyruvate Kinase M2 Inhibits CD4+ T Cell Pathogenicity and Suppresses Autoimmunity. Cell Metab, 31 (2): 391-405.e8. DOI: 10.1016/j.cmet.2019.10.015 [PMID:31761564] |
3. Fan F, Wood KV. (2007)
Bioluminescent assays for high-throughput screening. Assay Drug Dev Technol, 5 (1): 127-36. [PMID:17355205] |
4. Jiang J, Walsh MJ, Brimacombe KR, Anastasiou D, Yu Y, Israelsen WJ, Hong BS, Tempel W, Dimov S, Veith H et al.. (2010)
ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model. Probe Reports from the NIH Molecular Libraries Program,. [PMID:23905203] |
5. Jiang JK, Boxer MB, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW et al.. (2010)
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett, 20 (11): 3387-93. [PMID:20451379] |