Biological Information
Background Information:
PDHK1 (pyruvate dehydrogenase kinase 1) is a mitochondrial enzyme that regulates cellular metabolism by inhibiting the pyruvate dehydrogenase (PDH) complex. It phosphorylates and inactivates PDH, controlling pyruvate entry into the TCA cycle and balancing glycolysis and oxidative phosphorylation. Regulated by hormones, nutrients, and oxygen levels, PDHK1 is crucial for glucose homeostasis, energy production, and metabolic adaptation. As a key metabolic regulator, it's a potential therapeutic target for metabolic disorders, cancer, and other diseases characterized by aberrant cellular metabolism. PDHK1 enhancement may protect cognitive recovery, while its inhibition is associated with various disorders, including abnormal myelination, hypoglycemia, ketoacidosis, seizures, and peripheral neuropathy.
Family:
Kinase
Sub Family:
PDHK
Class:
Atypical
Protein Name:
PDHK1
Uniprot Number:
Q15118
Protein Aliases:
Pyruvate dehydrogenase kinase isoform 1 (PDH kinase 1)
Gene Name:
PDK1
Gene ID:
5163
Gene Aliases:
pyruvate dehydrogenase kinase, isoenzyme 1; pyruvate dehydrogenase kinase, isozyme 1
Accession Number:
NM_002610
Organism:
Human
Construct Details:
Full length, recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Luminescence
Measured Response:
Luminescence
Testing Information
Procedure Summary:
Human recombinant protein kinase PDHK1 expressed in Sf9 insect cells is used. Test compound and/or vehicle is preincubated with 4 μg/ml enzyme in modified Tris-HCl buffer pH 7.4 for 15 minutes at 37˚C. The reaction is initiated by addition of 200 μg/ml PDHKtide and 10 μM ATP for another 90- minute incubation period and terminated by ADP-GloTM Reagent. Read luminescence on a spectrophotometer after adding Kinase Detection Regent. Compounds are screened at 10 μM.
Substrate:
200 mg/ml PDHKtide
ATP Concentration:
10 µM
Incubation:
90 min at 37˚C
Control Inhibitor:
VER-246608
Criteria For Significance:
≧ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
10
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei