Biological Information

Background Information:

Cathepsin B, L and H are lysosomal enzymes that belong to the papain superfamily of cysteine proteinases. They are thought to be involved in tumor invasion and metastasis. In addition, high levels of Cathepsin B have been found in the synovial fluid of rheumatoid arthritis patients which may degrade collagen. Inhibition of Cathepsin B may reduce inflammation, tumor growth and angiogenesis.

Family:

Protease

Sub Family:

Papain

Class:

Cysteine Peptidase

Protein Name:

Cathepsin B

Uniprot Number:

P07858

Gene Name:

CTSB

Gene ID:

1508

Accession Number:

NM_147780

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 B is used. Test compound and/or vehicle is incubated with 3.94 mU/ml enzyme‡ in modified acetate buffer pH 5.5 for 15 minutes at 25°C. The reaction is initiated by addition of and 20 μM Boc-Leu-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 Boc-Leu-Arg-Arg-AMC

Incubation:

30 min at 25°C

Control Inhibitor:

CA-074

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

9821383

Name

CA-074

Measurement

0.0048μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP326