Src Human TK Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW

Item: 176810

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Src family tyrosine kinases are nonreceptor tyrosine kinases that are functionally linked to some receptor-type tyrosine kinases, G-protein-coupled receptors, cytokine receptors, and cell adhesion molecules/receptors. Src family tyrosine kinases are membrane-associated proteins having Src homology 2 (SH2) and SH3 domains, which are important for protein-protein interaction. The activity of Src family tyrosine kinases is regulated through intramolecular interaction between the SH2 domain and the phosphorylated tyrosine at the C-terminal regulatory site (Tyr-527).

Family:

Kinase

Sub Family:

Class:

Protein Tyrosine

Protein Name:

Src

Uniprot Number:

P12931

Protein Aliases:

Proto-oncogene c-Src|pp60c-src|p60-Src

Gene Name:

SRC

Gene ID:

6714

Gene Aliases:

ASV|c-src

Accession Number:

NM_005417

Organism:

Human

Construct Details:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant protein kinase SRC expressed in insect cells is used. Test compound and/or vehicle is preincubated with 0.023 μg/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 37°C. The reaction is initiated by addition of 0.2 mg/ml poly(Glu:Tyr), 10 μM ATP and 0.05 μCi [γ³²P]ATP for another 30 minute incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [³²P]Poly(Glu:Tyr) formed. Compounds are screened at 10 μM.

Substrate:

200 µg/ml Poly(Glu:Tyr)

ATP Concentration:

10 uM

Incubation:

30 min at 37°C

Control Inhibitor:

Staurosporine

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

0.077μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Inhibition of SRC (p60-Src, c-src) may be useful in the treatment of breast and colon carcinoma.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei