OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
CLK2 (CDC2-like kinases) proteins contain an Serine- and Arginine-rich (SR) domain and autophosphorylate on tyrosine, serine, and threonine residues in overexpression systems and in vitro. Mutations in the clk-2 gene of the nematode Caenorhabditis elegans affect organismal features such as development, behavior, reproduction, and aging as well as cellular features such as the cell cycle, apoptosis, the DNA replication checkpoint, and telomere length. These results suggest the existence of a novel class of protein kinases, with an unusual substrate specificity, which may be involved in cell cycle control. Overexpression of CLK2 decreases cell cycle length. Inhibition of CLK2 may reversibly arrest the cell cycle and tumor growth.
Family:
Kinase
Sub Family:
CMGC
Class:
Protein Ser/Thr
Protein Name:
CLK2
Uniprot Number:
P49760
Protein Aliases:
CDC-like kinase 2
Gene Name:
CLK2
Gene ID:
1196
Accession Number:
NM_003993
Organism:
Human
Construct Details:
138-end recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
CLK2 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 20 µM YRRAAVPPSPSLSRHSSPHQS(p) EDEEE, 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:
20 µM YRRAAVPPSPSLSRHSSPHQS(p) EDEEE
Tracer:
33P
ATP Concentration:
[ATP]= 15µM (Km= 24µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Staurosporine
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
Adverse / Beneficial Action:
Inhibition of CLK2 may reversibly arrest the cell cycle and tumor growth.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
CLK2 Human CMGC Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-774KP10
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