Cathepsin K Human Papain Cysteine Peptidase Enzymatic LeadHunter Assay - TW

Item: 112600

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OVERVIEW

DOCUMENTS/REFERENCES

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 K is highly and selectively expressed in osteoclasts, closely involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Inhibitors of cathepsin K are in development for treatment of osteoporosis and other disease targets such as osteoarthritis and bone metastasis.

Family:

Protease

Sub Family:

Papain

Class:

Cysteine Peptidase

Protein Name:

Cathepsin K

Uniprot Number:

P43235

Gene Name:

CTSK

Gene ID:

1513

Gene Aliases:

PKND

Accession Number:

NM_000396

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 K expressed in insect cells is used. Test compound and/or vehicle is incubated with 0.02 µg/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 25⁰C. The reaction is initiated by addition of 10 µM Z-Phe-Arg-AMC for another 30 minutes incubation period. Determination of the amount of AMC formed is read spectrofluorimetrically at 360/465 nm. Compounds are screened at 10 µM.

Substrate:

10 µM Z-Phe-Arg-AMC

Incubation:

30 min at 25°C

Control Inhibitor:

Odanacatib

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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

10152654

Name

Odanacatib

Measurement

0.00052μM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei