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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei