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 components of signal transduction pathways and regulate cell growth, division and differentiation, and the activities of a variety of oncoproteins and transcription factors. CSNK1D (Casein kinase I delta isoform, CKI-delta, CKId) 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:

CK1delta

Uniprot Number:

P48730

Protein Aliases:

CKId|Tau-protein kinase CSNK1D

Gene Name:

CSNK1D

Gene ID:

1453

Gene Aliases:

HCKID|CKID|CKIdelta

Accession Number:

AB063114

Organism:

Human

Construct Details:

1-294 recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

CK1d (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= 77µM )

Incubation:

40 min at Room temperature

Control Inhibitor:

PKR Inhibitor

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

6490494

Name

PKR Inhibitor

Measurement

185.7nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault

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Item: 14-520KP