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
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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