Biological Information
Background Information:
Mammalian casein kinase 1 (CK1) gene family consists of seven different genes in mammals, CKIa, b, g1, g2, g3, d and e. These enzymes are important component of signal transduction pathways, regulates cell growth, division and differentiation, and the activities of a variety of oncoproteins and transcription factors. CSNK1G1 (Casein kinase I gamma1 isoform) plays an important role in cell survival and protects regulatory proteins from caspase-mediated degradation in apoptosis. Inhibitors may find clinical use for the treatment of Alzheimer’s disease and amyotrophic lateral sclerosis.
Family:
Kinase
Sub Family:
CK1
Class:
Protein Ser/Thr
Protein Name:
CK1gamma1
Uniprot Number:
Q9HCP0
Protein Aliases:
Casein kinase I isoform gamma-1|CKI-gamma 1
Gene Name:
CSNK1G1
Gene ID:
53944
Gene Aliases:
CK1gamma1
Accession Number:
NM_022048
Organism:
Human
Construct Details:
25-355 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
CK1g1 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 µM KRRRALS(p)VASLPGL, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 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 methanol prior to drying and scintillation counting.
Substrate:
200 µM KRRRALS(p)VASLPGL
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 22.91µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Cdk1/2 Inhibitor III
Test Sample Requirements:
Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.
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.
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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