DASA-58

DASA-58 is a selective activator of pyruvate kinase M2 (PKM2) (AC₅₀ = 38 nM). DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated protein. In cancer, the altered glucose metabolism can be influenced by the regulatory properties of PKM2.