CHK2 (CHEK2) (I157T) Human CAMK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR

Item: 14-741KP10

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Checkpoint kinase (CHK) is activated by a broad spectrum of DNA-damaging agents, including DNA-strand-breaking agents such as ionizing radiation and topoisomerase inhibitors, and those agents that cause replication stress such as ultraviolet light, hydroxyurea and 5-fluorouracil. CHK2 might have a redundant and supportive role in checkpoints, but its role in ionizing radiation-induced apoptosis is more prominent. However, its role in other DNA-damage-induced apoptosis mechanisms is less well established. CHK2 inhibitors are expected to sensitize proliferating cells to chemotherapy-induced apoptosis.

Family:

Kinase

Sub Family:

CAMK

Class:

Protein Ser/Thr

Protein Name:

CHK2

Uniprot Number:

O96017

Protein Aliases:

CHK2 checkpoint homolog|Cds1 homolog|Hucds1|hCds1|Checkpoint kinase 2

Gene Name:

CHEK2

Gene ID:

11200

Gene Aliases:

CDS1|CHK2|HuCds1|PP1425|bA444G7|RAD53

Accession Number:

NP_009125

Organism:

Human

Construct Details:

5-end; I157T recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

CHK2 (I157T) (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 µM KKKVSRSGLYRSPSMPENLNRPR, 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:

100 µM KKKVSRSGLYRSPSMPENLNRPR

Tracer:

33P

ATP Concentration:

[ATP]= 10µM (Km= 179.7µM )

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:

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

62.34nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault