Biological Information

Background Information:

Caspases 9 is a member of the CED-3/caspase-3 subfamily. Upon activation, it functions to activate downstream effector caspases in the apoptotic pathway. 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 9

Uniprot Number:

P55211

Protein Aliases:

protein phosphatase 1, regulatory subunit 56

Gene Name:

CASP9

Gene ID:

842

Gene Aliases:

MCH6|ICE-LAP6|APAF-3|PPP1R56

Accession Number:

NM_032996

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 9 expressed in E. coli is used. Test compound and/or vehicle is preincubated with 10.2 µg/mL enzyme in modified HEPES buffer pH 7.4 for 15 minutes at 37°C. The reaction is initiated by addition of 25 µM Ac-LEHD-AFC for another 60 minutes 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-LEHD-AFC

Incubation:

60 min at 37°C

Control Inhibitor:

Ac-LEVD-CHO

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

11225800

Name

Ac-LEVD-CHO

Measurement

0.26μM - IC50

PubChem ID

44135117

Name

Ac-IETD-CHO

Measurement

4.2μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP325