Pyruvate 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).Unlike other eukaryotic protein kinases, PDHK is a member of a family of mitochondrial protein kinases. By phosphorylating three seryl residues in the pyruvate dehydrogenase moiety, PDHK inactivates the multienzyme mitochondrial pyruvate dehydrogenase complex and is a key player in the regulation of glucose homeostasis.
In humans, PDHK has four isoforms (numbered 1 to 4). PDHK isoforms are potential therapeutic targets for these significant human diseases because they are up-regulated in obesity, diabetes, heart failure, and cancer.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V1942 | AZD7545 | 252017-04-2 | AZD7545 is anovel, potent, selective small-molecule inhibitor of PDHK (pyruvate dehydrogenase kinase 2) with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. |
|
V1911 | Dicoumarol (Dicumarol) | 66-76-2 | Dicoumarol (also named as Dicumarol) is an oral and competitive inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively. |
|
V23059 | JX-06 | 729-46-4 | JX06 is a potent, selective, covalent PDK inhibitor. |
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