Biological Information

Background Information:

Prolyl oligopeptidase (POP) is an intracellular enzyme (80kDa) that is highly conserved in mammals and is broadly distributed with high concentrations found in the brain. Inhibitors of POP are potentially useful in the treatment of infectious diseases and may have anti-amnesiac properties. On the other hand, inhibitors may promote neuronal degeneration in Alzheimer’s Disease and fibrosis in heart and kidney.

Family:

Protease

Class:

Serine Peptidase

Protein Name:

Prolyl endopeptidase

Uniprot Number:

P48147

Protein Aliases:

Post-proline cleaving enzyme

Gene Name:

PREP

Gene ID:

5550

Gene Aliases:

prolyl oligopeptidase

Accession Number:

NM_002726

Organism:

Human

Construct Details:

Full length, recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetric

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant Prolyl Oligopeptidase/PREP expressed in Sf21 cells is used. Test compound or vehicle is preincubated with 0.068 μg/ml enzyme in Tris-HCl buffer pH 7.5 for 15 minutes at 25°C. The reaction is initiated by addition of 50 μM Z-Gly-Pro-AMC for another 30-minute incubation period. Determination of the amount of AMC formed is read spectrofluorimetrically at excitation 380 nm and emission 460 nm. Compounds are screened at 10 μM.

Substrate:

50 μM Z-Gly-Pro-AMC

Incubation:

30 min at 25°C

Control Inhibitor:

KYP 2047

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

Name

Z-Pro-Pro-aldehyde-dimethyl acetal

Measurement

4.7μM - IC50

PubChem ID

11198569

Name

KYP 2047

Measurement

0.00027μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei