Biological Information
Background Information:
Cathepsin B, L and H are lysosomal enzymes that belong to the papain superfamily of cysteine proteinases. Cathepsin L is one of the most active cysteine proteases and accounts for most of the lysosomal cysteine protease activity. It has been implicated in a range of processes including turnover of proteins involved in growth regulation, tumor invasion and metastasis, and bone resorption as well as degradation of collagen and elastase. Inhibition of Cathepsin L may reduce tumor growth, angiogenesis, invasion and metastasis, rheumatoid arthritis and other inflammatory diseases as well as emphysema.
Family:
Protease
Sub Family:
Papain
Class:
Cysteine Peptidase
Protein Name:
Cathepsin L
Uniprot Number:
P07711
Gene Name:
CTSL
Gene ID:
1514
Gene Aliases:
FLJ31037
Accession Number:
NM_001912
Organism:
Human
Construct Details:
Endogenous
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human liver cathepsin L is used. Test compound and/or vehicle is incubated with 0.061 mU/ml enzyme‡ in modified acetate buffer pH 5.5 for 15 minutes at 25⁰C. The reaction is initiated by addition of 20 μM Z-Phe-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:
20 µM Z-Phe-Arg-AMC
Incubation:
30 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
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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