DASA-58
DASA-58 is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).{21504} DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins.{21504} Through its effects on PKM2, DASA-58 blocks the induction of HIF-1? by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1?-dependent targets, including IL-1?.{31878} It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.{31877}
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