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). The subcellular mechanism of DUSP10 is unique in being present in both the cytoplasm and nucleus. Further, DUSP10 blocks the enzymatic activation of MAP kinases with a high selectivity for p38 and JNK/SAPK relative to MAPK/ERK, which are associated with cellular proliferation and differentiation.
Family:
Phosphatase
Sub Family:
Dual Specificity
Class:
Protein Tyrosine
Protein Name:
MKP5
Uniprot Number:
Q9Y6W6
Gene Name:
DUSP10
Gene ID:
11221
Gene Aliases:
MKP-5|MKP5
Accession Number:
NM_007207
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-5 expressed in insect Sf9 cells is used. Test compound and/or vehicle is preincubated with 0.05 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 DUSP10 may facilitate progression of prostatic inflammation and prostate cancer.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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