RSK3 Human AGC Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR

Item: 14-462KP10

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Serine/threonine protein kinases RSKs contain three isoforms RSK1, RSK2 and RSK3 and act at the distal end of MAPK signalling pathway. They are directly phosphorylated and activated by ERK1/2 in response to many growth factors, peptide hormones and neurotransmitters. RSKs have been shown to regulate apoptosis through phosphorylation and inactivation of the pro-apoptotic protein BAD, and cell cycle since the kinase Myt1 is a RSK target. RSK3 (Ribosomal protein S6 kinase 3, SK6-alpha, MAPKAPK1C) is especially interesting, because it features an additional nuclear targetting signal near its N-terminus, and can phosphorylate a variety of transcription factors (CREB, TCF/Lef, Myc, the estrogen receptor, and the Fos subunit of AP-1).

Family:

Kinase

Sub Family:

AGC

Class:

Protein Ser/Thr

Protein Name:

RSK3

Uniprot Number:

Q15349

Protein Aliases:

Gene Name:

RPS6KA2

Gene ID:

6196

Gene Aliases:

RSK|RSK3|HU-2|MAPKAPK1C

Accession Number:

XM_004469

Organism:

Human

Construct Details:

Full length recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Rsk3 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 µM KKKNRTLSVA, 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:

30 uM KKKNRTLSVA

Tracer:

33P

ATP Concentration:

[ATP]= 10µM (Km= 7µM )

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:

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

122130844

Name

Staurosporine

Measurement

0.75nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Inhibition of RSK3 may be useful in the treatment of tumor cell metastasis.

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault