PDHK
Pyruvate dehydrogenase kinase; PDH kinase
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). 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.
There 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.
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PDHK Related Products (38)
Related Products (38)
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Antibodies (1)
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DHNA
0 ImagesSynonyms: 1,4-Dihydroxy-6-naphthoic acidDHNA (KIS20) is a PDH kinase 4 (PDK4) inhibitor with an IC50 of 18 μM. DHNA can be used for the study of heart failure.
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PDHc-E2-IN-1
0 ImagesCat. No.: HY-176997CAS No.: 3031881-21-4PDHc-E2-IN-1 (Compound 9) is a Pyruvate Dehydrogenase Complex E2 (PDHc-E2) inhbibitor. with an IC50 of 2.52 μM. PDHc-E2-IN-1 shows strong antibacterial activity and can be used in the research of bacterial spot disease and bacterial leaf blight in rice.
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PDK-IN-2
0 ImagesCat. No.: HY-156109CAS No.: 3032446-61-7PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model.
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Dicoumarol-d8
0 ImagesCat. No.: HY-N0645SCAS No.: 2469035-18-3Synonyms: Dicumarol-d8Dicoumarol-d8 (Dicumarol-d8) is the deuterium labeled Dicoumarol. Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.
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(S)-CPP
0 ImagesCat. No.: HY-W110242CAS No.: 41998-38-3(S)-CPP is an allosteric BDK inhibitor. (S)-CPP can be used in the research of type 2 diabetes.
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PDHK-IN-5
0 ImagesCat. No.: HY-146554PDHK-IN-5 (Compound 19) is a potent inhibitor of PDHK with IC50s of 0.006 and 0.0329 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases.
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Arachidonic acid leelamide
0 ImagesCat. No.: HY-173581CAS No.: 2841710-23-2Arachidonic acid leelamide, a Leelamine (HY-W005629) analog, is a pyruvate dehydrogenase kinase (PDK) inhibitor. Arachidonic acid leelamide can be used for the study of breast cancer.
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PDK4-IN-2
0 ImagesCat. No.: HY-157538CAS No.: 1616752-12-5PDK4-IN-2 (compound 8) is a pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 of 46 µM. PDK4-IN-2 improves ejection fraction of failing hearts by regulating bioenergetics via activation of the tricarboxylic acid cycle.
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Pipcroside C
0 ImagesCat. No.: HY-N15518Pipcroside C is found in P. crocatum Ruiz & Pav. Pipcroside C is a PDH inhibitor (IC50: 80.25 µM). Pipcroside C has antibacterial activity and is used in the study of oral infections.
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PDHK1-IN-3
0 ImagesCat. No.: HY-173301PDHK1-IN-3 (Compound 29) is a selective PDHK1 inhibitor with an IC50 of 0.028 μM against PDHK1 and an IC50 of 0.120 μM against PDHK2. PDHK1-IN-3 inhibits the activity of PDHK1 by forming a covalent bond with Lys299 in PDHK1. PDHK1-IN-3 can be used in the research of autoimmune diseases, inflammatory diseases, and cancer.
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PDHK1-IN-1
0 ImagesCat. No.: HY-170838PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 (IC50=1.5 μM) with anticancer activity. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), limiting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 can shift the metabolism towards an increased glycolysis dependence (Warburg effect). PDHK1-IN-1 can inhibit the phosphorylation of the PDC E1α Ser232 recognition site of PDHK1 and the phosphorylation of Ser293.
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Pipcroside B
0 ImagesCat. No.: HY-N15517Pipcroside B is found in P. crocatum Ruiz & Pav. Pipcroside B is a PDH inhibitor (IC50: 99.82 µM). Pipcroside B has antibacterial activity and is used in the study of oral infections.
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PDHK-IN-7
0 ImagesCat. No.: HY-162586CAS No.: 1220965-73-0PDHK-IN-7 (compound 32) is an inhibitor of pyruvate dehydrogenase kinase with an IC50 value of 17 nM.PDHK-IN-7 activates PDH in rat livers and has a glucose-lowering effect in Zucker fatty rats.
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PDHK1-IN-2
0 ImagesCat. No.: HY-173298CAS No.: 2870691-38-4PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinases 1/2 (PDHK1/2), with an IC50 of 0.007 μM for PDHK1 and an IC50 of 0.015 μM for PDHK2. PDHK1-IN-2 can regulate immune cell metabolism and correct mitochondrial dysfunction, and is expected to be used in the research of autoimmune diseases, inflammatory diseases, cancers, and other conditions.
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