PKM 活化剂;PKM Activators;;InformationDASA-58 DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.TargetsPKM2In vitroDASA-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 vivoDASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice.