Biological Information
Background Information:
SYK tyrosine kinase (spleen tyrosine kinase) is a key molecule in the development of the B cell lineage and the activation of B lymphocytes after Ag recognition by the B-cell receptor. Syk binds to ITAM motifs and initiates signaling pathway such as Ras, PI3 Kinase, Ca2+ flux , and PLCγ2. SYK is required for early B cell development.
Family:
Kinase
Sub Family:
TK
Class:
Protein Tyrosine
Protein Name:
Syk
Uniprot Number:
P43405
Protein Aliases:
Spleen tyrosine kinase|p72-Syk
Gene Name:
SYK
Gene ID:
6850
Accession Number:
NM_001135052
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 SYK expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.18 U/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 37°C. The reaction is initiated by addition of 200 µg/ml poly(Glu:Tyr), 10 µM ATP and 0.25 µCi [γ-32P]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:
10
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Inhibition of SYK may be useful in the treatment of inflammatory and alledrgy diseases such as asthma. Inhibition of SYK may, however, promote metastasis in human gastric cancer.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei