Biological Information

Background Information:

MST1 and MST2 contain a putative caspase cleavage site at the junction of the catalytic domain and the C-terminal region. MST is involved in a positive feedback loop in possible association with the SAPK and p38-MAPK pathways. MST1 has been shown activated in cellular apoptosis induced by a variety of stimuli. Inhibition of MST1 may inhibit Raf-1-mediated cell proliferation and result in apoptosis.

Family:

Kinase

Sub Family:

STE

Class:

Protein Ser/Thr

Protein Name:

MST1

Uniprot Number:

Q13043

Protein Aliases:

mammalian sterile 20-like 1|yeast Ste20-like|kinase responsive to stress 2

Gene Name:

STK4

Gene ID:

6789

Gene Aliases:

MST1|KRS2|YSK3

Accession Number:

NM_006282

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:

MST1 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 µM KKSRGDYMTMQIG, 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:

250 uM KKSRGDYMTMQIG

Tracer:

33P

ATP Concentration:

[ATP]= 90µM (Km= 102µM )

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

PubChem ID

122130844

Name

Staurosporine

Measurement

1.61nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault

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