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

PubChem ID

329755181

Name

Endothall

Measurement

0.59μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP260