Biological Information

Background Information:

Caspases 5 is a member of the caspase 1 subfamily involved in Fas-mediated apoptosis. Cleavage sites of caspase 5 are located at asp311 and asp330, and possibly asp121. Caspase inhibitors are currently sought as therapeutics for such diseases as Alzheimer's, Parkinson's and cerebral/myocardial ischemia.

Family:

Protease

Sub Family:

Caspase

Class:

Cysteine Peptidase

Protein Name:

Caspase 5

Uniprot Number:

P51878

Gene Name:

CASP5

Gene ID:

838

Gene Aliases:

ICE(rel)III

Accession Number:

NM_004347

Organism:

Human

Construct Details:

Fragment, 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 caspase 5 expressed in E. coli is used. Test compound and/or vehicle is preincubated with 300 U/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 37⁰C. The reaction is initiated by addition of 25 μM Ac-WEHD-AFC for another 60 minute incubation period. Determination of the amount of AFC formed is read spectrofluorimetrically at 400 nm/510 nm. Compounds are screened at 10 μM.

Substrate:

25 µM Ac-WEHD-AFC

Incubation:

60 min at 37°C

Control Inhibitor:

Z-WEHD-FMK

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

644345

Name

Ac-DEVD-CHO

Measurement

1.5μM - IC50

PubChem ID

5311139

Name

Ac-YVAD-CHO

Measurement

3.8μM - IC50

PubChem ID

11225800

Name

Ac-LEVD-CHO

Measurement

0.14μM - IC50

PubChem ID

15487887

Name

Ac-VEID-CHO

Measurement

2.1μM - IC50

PubChem ID

25108684

Name

Z-VDVAD-FMK

Measurement

3.2μM - IC50

PubChem ID

44135117

Name

Ac-IETD-CHO

Measurement

2.6μM - IC50

PubChem ID

122173007

Name

Z-LEHD-fmk

Measurement

1.2μM - IC50

PubChem ID

Name

Z-WEHD-FMK

Measurement

0.34μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP325