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. DUSP4 is localized within the cell nucleus and reported to be expressed in placenta and pancreas.

Family:

Phosphatase

Sub Family:

Dual Specificity

Class:

Protein Tyrosine

Protein Name:

MKP2

Uniprot Number:

Q13115

Protein Aliases:

VH1 homologous phosphatase 2|MAP kinase phosphatase 2

Gene Name:

DUSP4

Gene ID:

1846

Gene Aliases:

HVH2|MKP-2|TYP

Accession Number:

NM_001394

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-2 expressed in insect Sf9 cells is used. Test compound and/or vehicle is preincubated with 1.2 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

PubChem ID

5154

Name

Sanguinarine

Measurement

8.1μM - IC50

PubChem ID

379077

Name

NSC 663284

Measurement

3.8μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

Inhibition of DUSP4 may facilitate hepatic gluconeogenesis.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei