OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Kinase that plays a key role in regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress.
Family:
Kinase
Sub Family:
Other (PDHK)
Class:
Protein Ser/Thr
Protein Name:
PDK1
Uniprot Number:
Q15118
Protein Aliases:
Pyruvate dehydrogenase kinase isoform 1 (PDH kinase 1)
Gene Name:
PDK1
Gene ID:
5163
Gene Aliases:
PDHK1
Accession Number:
NM_002610.3
Organism:
Human
Construct Details:
Full length recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
PDHK1 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 µM KKKYHGHSMSDPGVSYRT, 10 mM Magnesium acetate and [γ-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 120 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in ethanol prior to drying and scintillation counting.
Substrate:
250 µM KKKYHGHSMSDPGVSYRT
Tracer:
33P
ATP Concentration:
[ATP]= 90µM (Km= 96.1µM )
Incubation:
120 min at Room temperature
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 50X stock based on the top concentration to be tested -OR- 100 μl of 10 mM stock -OR- 1.5 mg (pre-weighed). 2) Dose Response: 80 μl of 50X stock based on the top concentration to be tested -OR- 100 μl of 10 mM stock -OR- 1.5 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
6 Business Days
Service Scheduling Note:
Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
KinaseProfiler
Testing Location:
KP - France - Celle L'Evescault
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