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. Increase in Cathepsin H expression has been detected in human endometrium during the proliferative phase of the menstrual cycle, injured tissue as well as in several tumors. Cathepsin H has also been reported to transform LDL to an atherogenic moiety. Inhibition of Cathepsin H may impair tumor growth and invasion as well as reduce atherogenesis.
Family:
Protease
Sub Family:
Papain
Class:
Cysteine Peptidase
Protein Name:
Cathepsin H
Uniprot Number:
P09668
Gene Name:
CTSH
Gene ID:
1512
Gene Aliases:
ACC-4|ACC-5|ACC4|ACC5
Accession Number:
NM_004390
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 H is used. Test compound and/or vehicle is preincubated with 3.3 mU/ml enzyme‡ in sodium acetate buffer pH 5.5 for 15 minutes at 25⁰C. The reaction is initiated by addition of 20 μM L-Arg-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 L-Arg-AMC
Incubation:
30 min at 25°C
Control Inhibitor:
E-64
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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