Biological Information

Background Information:

Phosphatase PP1a, isoform of protein phosphatase type 1 (PP1), is a major eukaryotic serine/threonine protein phosphatase involved in regulation of numerous cell functions such as cell division, transcription, translation, muscle contraction, glycogen synthesis, and signal transduction pathways in cooperation with protein kinases. Inhibition of PP1 has been shown to either induce or inhibit apoptosis in several cell types and suggested to be capable of modulating protein phosphorylation for the treatment, amelioration or prevention in various pathological situations, including degenerative diseases and cancers.

Family:

Phosphatase

Class:

Protein Ser/Thr

Protein Name:

PP1alpha

Uniprot Number:

P62136

Gene Name:

PPP1CA

Gene ID:

5499

Gene Aliases:

PP1A|PP-1A|PP1alpha

Accession Number:

NM_002708

Organism:

Human

Construct Details:

Full Length, 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 PP1α expressed in E. cole cells is used. Test compound and/or vehicle are preincubated with 0.8 μg/ml‡ of enzyme for 15 minutes at 25⁰C in Hepes buffer pH 7.0. The reaction is initiated by addition of 250 µM DiFMUP for another 30 minute incubation period. Read plate on a spectrophotometer (Excitation: 355nm, Emission: 460 nm). Compounds are screened at 10 μM.

Substrate:

250 µM DiFMUP

Incubation:

30 min at 25°C

Control Inhibitor:

Microcystin-LR

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

5944

Name

Cantharidin

Measurement

0.3μM - IC50

PubChem ID

445434

Name

Microcystin-LR

Measurement

0.009μM - IC50

PubChem ID

329755181

Name

Endothall

Measurement

6.4μM - IC50

PubChem ID

179202

Name

Calyculin A

Measurement

0.004μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP260