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

PubChem ID

173830

Name

L-Leu-Chloromethylketone

Measurement

>100μM - IC50

PubChem ID

299927

Name

Z-Gly-Leu-Phe-CMK

Measurement

0.00061μM - IC50

PubChem ID

7098622

Name

Leupeptin

Measurement

0.00016μM - IC50

PubChem ID

11957542

Name

E-64

Measurement

0.067μM - IC50

PubChem ID

16760356

Name

Cathepsin Inhibitor I

Measurement

0.33μM - IC50

PubChem ID

16760357

Name

Cathepsin Inhibitor II

Measurement

0.18μM - IC50

PubChem ID

46936189

Name

Chymostatin

Measurement

0.012μM - IC50

PubChem ID

Name

Gly-Phe-CHN2

Measurement

3.8μM - IC50

PubChem ID

6918602

Name

Relacatib

Measurement

0.0025μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP326