Biological Information
Background Information:
Protein phosphatase 2A (PP2A) is involved in the regulation of cell growth and intracellular signal transduction pathways. For example, over-expression of the catalytic subunit of protein PP2A has been reported to increase the basal activity of the HIV-1 viral promoter and PP2A activity has been implicated in the inhibition of c-Jun N-terminal kinase (JNK). The dual regulatory function of PP2A as both inhibitor and activator may result from the formation and activity of different multimeric PP2A complexes within distinct subcellular locations. PP2A inhibitors have potential therapeutic utility in the treatment of inflammation, cancer and HIV-AIDS.
Family:
Phosphatase
Class:
Protein Ser/Thr
Protein Name:
PP2A
Uniprot Number:
P67775
Protein Aliases:
protein phosphatase 2A catalytic subunit, alpha isoform
Gene Name:
PPP2CA
Gene ID:
5515
Gene Aliases:
PP2Calpha
Accession Number:
NM_002715
Organism:
Human
Construct Details:
Fragment (catalytic domain)
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrofluorimetry
Platform:
Plate reader
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant protein phosphatase PP2Aexpressed in insect cells is used. Test compound and/or vehicle is preincubated with 0.292 µg/ml enzyme for 15 minutes at 37°C in modified HEPES buffer pH 7.2. The reaction is initiated by addition of 100 µM DiFMUP for 30 minutes. Determination of the amount of DiFMU formed is read spectrofluorimetrically at 358 nm/450 nm. Compounds are screened at 10 µM
Substrate:
100 µM DiFMUP
Incubation:
30 min at 37°C
Control Inhibitor:
Endothall
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
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS