MKP3 Human Phosphatase Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
The protein encoded by this gene is a member of the dual specificity protein phosphatase subfamily. These phosphatases inactivate their target kinases by dephosphorylating both the residues of phosphoserine/threonine and phosphotyrosine. They negatively regulate members of the mitogen-activated protein (MAP) kinase superfamily (MAPK/ERK, SAP/JNK, p38), especially ERK1 and ERK2, which are associated with cellular proliferation and differentiation. Different members of the family of dual specificity phosphatases show distinct substrate specificities for various MAP kinases, different tissue distribution and subcellular location. DUSP6 is reported to act as a suppressor in human pancreatic cancer.
Family:
Phosphatase
Sub Family:
Dual Specificity
Class:
Protein Tyrosine
Protein Name:
MKP3
Uniprot Number:
Q16828
Gene Name:
DUSP6
Gene ID:
1848
Gene Aliases:
MKP-3|PYST1
Accession Number:
NM_001946
Organism:
Human
Construct Details:
Full Length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant protein phosphatase MKP-3 expressed in insect Sf9 cells is used. Test compound and/or vehicle is preincubated with 2 μg/ml enzyme‡ for 15 minutes at 37°C in modified Tris-HCl buffer pH 7.2. The reaction is initiated by addition of 100 μM DiFMUP for 60 minutes. Determination of the amount of DiFMU formed is read spectrofluorimetrically at 358 nm/450 nm. Compounds are screened at 10 µM.
Substrate:
100 µM DiFMUP
Incubation:
60 min at 37°C
Control Inhibitor:
NSC 663284
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
Adverse / Beneficial Action:
Inhibition of DUSP6 may facilitate development of pancreatic cancer, especially pancreatic ductal adenocarcinoma.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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