Biological Information

Background Information:

Cathepsin E (E.C.3.4.23.34) is an intracellular non-lysosomal enzyme, aspartic peptidase of the pepsin family and has a limited cell and tissue distribution such as stomach, lymphoid tissues and urinary bladder. The presence of an N-linked oligosaccharide on cathepsin E indicates that it is glycosylated in the rough ER. Cathepsins D and E play an important role in the degradation of proteins, the generation of bioactive proteins, and antigen processing. Both enzymes are efficient in cleaving Swedish mutant of amyloid precursor protein (APP) at the b site but show almost no reactivity with wide-type APP. Inhibitors of cathepsin E may be immune suppressant.

Family:

Protease

Sub Family:

Pepsin

Class:

Aspartic Peptidase

Protein Name:

Cathepsin E

Uniprot Number:

P14091

Gene Name:

CTSE

Gene ID:

1510

Accession Number:

NM_001910

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 cathepsin E expressed in a murine myeloma NS0 cells is used. Test compound and/or vehicle is preincubated with 330 ng/ml enzyme‡ in modified acetate buffer pH 3.5 for 15 minutes at 25°C. The reaction is initiated by addition of 5 μM Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 for another 15 minute incubation period. Determination of the amount of Mca-Pro-Leu-Gly formed is read spectrofluorimetrically at 340 nm/400 nm. Compounds are screened at 10 μM.

Substrate:

5 µM Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH₂

Incubation:

15 min at 25°C

Control Inhibitor:

Pepstatin

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

299927

Name

Z-Gly-Leu-Phe-CMK

Measurement

47μM - IC50

PubChem ID

5478883

Name

Pepstatin

Measurement

0.00070μM - IC50

PubChem ID

7098622

Name

Leupeptin

Measurement

>10μM - IC50

PubChem ID

11957542

Name

E-64

Measurement

>10μM - IC50

PubChem ID

16760356

Name

Cathepsin Inhibitor I

Measurement

43μM - IC50

PubChem ID

16760357

Name

Cathepsin Inhibitor II

Measurement

18μM - IC50

PubChem ID

46936189

Name

Chymostatin

Measurement

>10μM - IC50

PubChem ID

Name

Gly-Phe-CHN2

Measurement

>10μM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP326