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

PubChem ID

5330812

Name

Cdk1/2 Inhibitor III

Measurement

44.08nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault

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Item: 14-711KP