Biological Information

Background Information:

Cathepsin B, H, K, L and S are lysosomal cysteine proteases and participate in a variety of proteolytic processes, including degradation of the extracellular matrix. Cathepsin S (EC 3.4.22.27 ) is highly expressed in lymph nodes, spleen, and antigen-presenting cells, including B lymphocytes, macrophages, and dendritic cells. Cathepsin S mediates degradation of the MHC class II invariant chain Ii and participates in antigen processing. Cathepsin S is also present during both the proliferative and secretory phases of the menstrual cycle. Inhibition of cathepsin S may be useful for immunosuppresive therapy of allergies or autoimmune diseases as well as tumors.

Family:

Protease

Sub Family:

Papain

Class:

Cysteine Peptidase

Protein Name:

Cathepsin S

Uniprot Number:

P25774

Gene Name:

CTSS

Gene ID:

1520

Accession Number:

NM_004079

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 S expressed in a murine myeloma NS0 cells is used. Test compound and/or vehicle is preincubated with 0.0604 μg/ml enzyme‡ in modified acetate buffer pH 4.5 for 15 minutes at 25°C. The reaction is initiated by addition of 10 μM Z-Leu-Arg-AMC for another 30 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:

30 min at 25°C

Control Inhibitor:

LY3000328

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

0.00031μM - IC50

PubChem ID

5478883

Name

Pepstatin

Measurement

>10μM - IC50

PubChem ID

7098622

Name

Leupeptin

Measurement

0.011μM - IC50

PubChem ID

11957542

Name

E-64

Measurement

0.0060μM - IC50

PubChem ID

16760356

Name

Cathepsin Inhibitor I

Measurement

0.17μM - IC50

PubChem ID

16760357

Name

Cathepsin Inhibitor II

Measurement

0.041μM - IC50

PubChem ID

46936189

Name

Chymostatin

Measurement

0.027μM - IC50

PubChem ID

Name

Gly-Phe-CHN2

Measurement

5.4μM - IC50

PubChem ID

67475270

Name

LY3000328

Measurement

0.086μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP326