Biological Information

Background Information:

Cathepsin V (also known as cathepsin L2 and U) is a cysteine protease of the papain family. It is expressed as a proenzyme in lysosomes, which can be autocatalytically converted to the mature form at pH 4.0. Cathepsin V shows high amino acid identity with cathepsin L. However, cathepsin V is specifically expressed in the thymus, testis, and corneal epithelium. Cathepsin V may play a significant role in thymic MHC class II antigen presentation and may be involved in autoimmune disease. Inhibition of Cathepsin V may prevent progression of myesthenia gravis and other autoimmune diseases.

Family:

Protease

Sub Family:

Papain

Class:

Cysteine Peptidase

Protein Name:

Cathepsin V

Uniprot Number:

O60911

Gene Name:

CTSV

Gene ID:

1515

Gene Aliases:

CTSU

Accession Number:

NM_001333

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 L2 expressed in a murine myeloma NS0 cells is used. Test compound and/or vehicle is preincubated with 36.2 ng/ml enzyme‡ in modified MES buffer pH 5.5 for 15 minutes at 25°C. The reaction is initiated by addition of 10 μM Z-Leu-Arg-AMC for another 60 minute incubation period. Determination of the amount of AMC formed is read spectrofluorimetrically at 360 nm/465 nm. Compounds are screened at 10 μM.

Substrate:

10 µM Z-Leu-Arg-AMC

Incubation:

60 min at 25°C

Control Inhibitor:

Relacatib

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

0.017μM - IC50

PubChem ID

7098622

Name

Leupeptin

Measurement

0.011μM - IC50

PubChem ID

11957542

Name

E-64

Measurement

0.089μM - IC50

PubChem ID

16760356

Name

Cathepsin Inhibitor I

Measurement

0.087μM - IC50

PubChem ID

16760357

Name

Cathepsin Inhibitor II

Measurement

0.038μM - IC50

PubChem ID

46936189

Name

Chymostatin

Measurement

0.0097μM - IC50

PubChem ID

Name

Gly-Phe-CHN2

Measurement

>10μM - IC50

PubChem ID

6918602

Name

Relacatib

Measurement

0.0015μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP326