Biological Information

Background Information:

Dipeptidyl peptidase 4 (DPP4; DPP IV, CD26) is a serine exopeptidase that cleaves X-proline dipeptides from the N terminus of polypeptides. It is an intrinsic membrane glycoprotein anchored into the cell membrane by its N-terminal end. High levels of the enzyme are found in the brush-border membranes of the kidney proximal tubule and of the small intestine, but several other tissues also express the enzyme. It has been suggested that physiological concentrations of GLP-1 (glucagon-like peptide-1) are degraded by DPP IV and the inhibitors of DPP IV may be a useful adjunct in the management of type II diabetes. Inhibitors of DPP IV may also be useful in reducing immune responses (asthma) as well as inflammation.

Family:

Protease

Sub Family:

Prolyl Oligopeptidase

Class:

Serine Peptidase

Protein Name:

DPP4

Uniprot Number:

P27487

Protein Aliases:

ADABP 

Gene Name:

DPP4

Gene ID:

1803

Gene Aliases:

DPPIV

Accession Number:

NM_001935

Organism:

Human

Construct Details:

Fragment (29-766), 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 DPP IV expressed in insect cells is used. Test compound and/or vehicle are preincubated with 42.5 ng/ml‡ of enzyme for 10 minutes at 25⁰C in Tris buffer pH 7.4. The reaction is initiated by addition of 40 µM GP-AMC for another 10 minute incubation period. Read plate on a spectrophotometer (Excitation: 355 nm, Emission: 460 nm). Compounds are screened at 10 μM.

Substrate:

40 µM GP-AMC

Incubation:

10 min at 25°C

Control Inhibitor:

UNII-74P4VV90RU

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

5281605

Name

Baicalein

Measurement

59.5μM - IC50

PubChem ID

9818824

Name

UNII-74P4VV90RU

Measurement

0.0019μM - IC50

PubChem ID

71433965

Name

P32/98

Measurement

0.12μM - IC50

PubChem ID

Name

DPP1c

Measurement

0.057μM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP318