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 |
|---|---|---|---|---|
|
V115478 | (S)-CPP | 41998-38-3 | (S)-CPP is an allosteric BDK inhibitor. |
|
V129346 | Arachidonic acid leelamide | 2841710-23-2 | Arachidonic acid leelamide is a pyruvate dehydrogenase kinase (PDK) inhibitor. |
|
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. |
|
V133648 | DHNA | 117255-85-3 | DHNA is a PDH kinase 4 (PDK4) inhibitor with an IC50 of 18 μM. |
|
V117454 | JTT251 | 1627957-25-8 | JTT251 is a PDHK inhibitor. |
|
V23059 | JX-06 | 729-46-4 | JX06 is a potent, selective, covalent PDK inhibitor. |
|
V111066 | PDHc-E2-IN-1 | 3031881-21-4 | PDHc-E2-IN-1 (compound 9) is an inhibitor of pyruvate dehydrogenase complex E2 (PDHc-E2) with an IC50 value of 2.52 μM. |
|
V142358 | PDHK1-IN-1 | PDHK1-IN-1 is a selective PDHK1 inhibitor (IC50=1.5 μM) with anticancer activity. | |
|
V142359 | PDHK1-IN-2 | 2870691-38-4 | PDHK1-IN-2 is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinase 1/2 (PDHK1/2), with an IC50 of 0.007 μM against PDHK1 and 0.015 μM against PDHK2. |
|
V142360 | PDHK1-IN-3 | PDHK1-IN-3 is a selective PDHK1 inhibitor with an IC50 value of 0.028 μM for PDHK1 and 0.120 μM for PDHK2. | |
|
V85501 | PDK-IN-3 | ||
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V84574 | PDK4-IN-2 | 1616752-12-5 | |
|
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. |
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