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Pyruvate kinase is an enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP in glycolysis and plays a role in regulating cell metabolism. There are four mammalian pyruvate kinase isoforms (PKM1, PKM2, PKR, PKL), and each isoform has had multiple designations over time in the literature. The M2 isoform of pyruvate kinase (PKM2) supports anabolic metabolism and is expressed both in cancer and normal tissue. The enzymatic activity of PKM2 is allosterically regulated by both intracellular signaling pathways and metabolites; PKM2 thus integrates signaling and metabolic inputs to modulate glucose metabolism according to the needs of the cell.

Cat. No. Product Name CAS No. Information
H9318

Etavopivat

 		2245053-57-8

Etavopivat is a potent pyruvate kinase activator.
H6828

TEPP-46

 		1221186-53-3

A potent activator of PKM2 (pyruvate kinase M2) with IC50 of 92 nM; shows no activity on PKM1 in vitro; binds to PKM2 at the subunit interaction interface site that is distinct from that of the endogenous activator FBP; inhibits xenograft tumor growth and orally bioactive.
H6827

Mitapivat

 		1260075-17-9

Mitapivat (PKM2 activator 1020, AG-348) is?a first-in-class, allosteric activator of Pyruvate kinase (PK) with mean AC50 of 29 nM (PK-R), activates a spectrum of recombinant mutant PK-R enzymes (R532W, R510Q);?AG-348 can increase the activity of wild-type and mutant PK enzymes in biochemical assays and in patient red blood cells treated ex vivo; demonstrates enhanced glycolytic pathway activity in PK-deficient RBCs that contain a variety of mutations.

Other Indication
H6826

DASA-58

 		1203494-49-8

A potent activator of PKM2 (pyruvate kinase M2) with AC50 of 38 nM; shows no activity on PKM1 in vitro; binds to PKM2 at the subunit interaction interface site that is distinct from that of the endogenous activator FBP; inhibits LPS-induced HIF-1α and IL-1β, as well as the expression of a range of other HIF-1α-dependent genes.

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