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

PubChem ID

173830

Name

L-Leu-Chloromethylketone

Measurement

0.14μM - IC50

PubChem ID

299927

Name

Z-Gly-Leu-Phe-CMK

Measurement

10μM - IC50

PubChem ID

7098622

Name

Leupeptin

Measurement

13μM - IC50

PubChem ID

11957542

Name

E-64

Measurement

1μM - IC50

PubChem ID

16760356

Name

Cathepsin Inhibitor I

Measurement

24μM - IC50

PubChem ID

16760357

Name

Cathepsin Inhibitor II

Measurement

11μM - IC50

PubChem ID

46936189

Name

Chymostatin

Measurement

>100μM - IC50

PubChem ID

Name

Gly-Phe-CHN2

Measurement

>100μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP326