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
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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