DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ACTIVATOR
Mechanism of action
Activator of pyruvate kinase M1/2
Product Description
Information
DASA-58 DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
Targets
PKM2
In vitro
DASA-58 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes in primary BMDMs, and also inhibits glycolysis and the accumulation of succinate in LPS-activated macrophages. In PC3 cells, DASA-58 impairs stromal-induced EMT program by restoring PK activity and abrogating the nuclear translocation of PKM2, as well as its association with HIF-1α. DASA-58 also dramatically reduces (~6-fold) CAFs-induced lung metastases formation in PC3 cells.
In vivo
DASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice.
1.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][10.1021/op500134e]
2.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][10.1021/op500134e]
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G2221185