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
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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