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

PubChem ID

5154

Name

Sanguinarine

Measurement

28μM - IC50

PubChem ID

379077

Name

NSC 663284

Measurement

0.99μM - IC50

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

RELATED SOLUTIONS

Item: PP260