Potent activator of pyruvate kinase M2 (PKM2) (IC50
= 73 nM). Exhibits little or no activity against the pyruvate kinase isozymes PKM1, PKL and PKR.
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Identification of activators for the M2 isoform of human pyruvate kinase version 3.
Boxer et al.
Probe Reports from the Molecular Libraries Program, 2010;
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Jiang et al.