PDHK-Inhibitors-Modulators-生命科学试剂-MedChemExpress.pdf

PDHK Pyruvate dehydrogenase kinase; PDH kinase PPyruvate dehydrogenase is a catalyst for an irreversible step in the degradation of glucose and its activity is regulated by a highly specific protein kinase, pyruvate dehydrogenase kinase (PDHK/PDK). PDHK belongs to a family of mitochondrial protein kinases unique from other eukaryotic protein kinases. PDHK inactivates the multienzyme mitochondrial pyruvate dehydrogenase complex by the phosphorylation of three seryl residues in the pyruvate dehydrogenase moiety, and thus plays an important role in the control of glucose homeostasis./P PThere are four isoforms of PDHK (1 to 4) in humans. PDHK isoforms are up-regulated in obesity, diabetes, heart failure, and cancer and are potential therapeutic targets for these important human diseases./P www.MedChemE 1 PDHK Inhibitors AZD7545 Dicoumarol Cat. No.: HY-16082 (Dicumarol) Cat. No.: HY-N0645 AZD7545 is a potent, competitive, selective PDHK2 Dicoumarol is an inhibitor of both NAD(P)H:quinone (pyruvate dehydrogenase kinase 2) inhibitor with oxidoreductase 1 (NQO1) and PDK1 with IC50s of IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, 0.37 and 19.42 μM, respectively. respectively. Purity: 99.91% Purity: 99.59% Clinical Data: Launched Clinical Data: Launched Si