Biological Information

Background Information:

p59fyn is a member of the src-related gene family of non-receptor tyrosine kinases. Recent studies indicate that fyn kinase plays a critical role in mediating signal transduction through the T-cell receptor thereby initiating a signal transduction cascade leading to lymphokine secretion and cell proliferation. One of the earliest biochemical responses following T-cell receptor activation is an increase in tyrosine kinase activity and concomitant phosphorylation of several intracellular substrates. P59fyn kinase is an important mediator of this phosphorylation since it is physically associated with the T-cell receptor. Additional evidence supports the view that fyn participates in signal transduction pathways leading from multiple T-cell membrane proteins and hence may serve to integrate stimuli received from several independent receptor structures. In the case of the B-cell receptor, fyn is one of several kinases associated with the receptor and is activated following receptor cross-linking.

Family:

Kinase

Sub Family:

TK

Class:

Protein Tyrosine

Protein Name:

Fyn

Uniprot Number:

P06241

Protein Aliases:

Proto-oncogene Syn|Proto-oncogene c-Fyn|Src-like kinase|SLK|p59-Fyn

Gene Name:

FYN

Gene ID:

2534

Gene Aliases:

SYN|SLK|MGC45350

Accession Number:

XM_017010650

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 Fyn expressed in insect cells is used. Test compound and/or vehicle is preincubated with 0.14 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 0.25 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:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

0.023μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP89