PP2B Human Phosphatase Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Calcineurin is a Calcineurin is a Ca2+/calmodulin-dependent protein phosphatase found in many cell types. It has been recently shown to be a key signaling enzyme in T-lymphocyte activation. It is also a major intracellular target for immunosuppressants such as the cyclosporin A/cyclophyllin complex. Inhibition of calcineurin, PP2B may be immunosuppressant, improve allograft survival in solid organ transplantation as well as useful in the treatment of some inflammatory diseases.
Family:
Phosphatase
Class:
Protein Ser/Thr
Protein Name:
PP2B
Uniprot Number:
Q08209
Protein Aliases:
calcineurin A alpha|protein phosphatase 2B, catalytic subunit, alpha isoform
Gene Name:
PPP3CA
Gene ID:
5530
Gene Aliases:
CNA1|PPP2B
Accession Number:
NM_000944 + NM_000945
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 protein phosphatase PP2B expressed in E. coli is used. Test compound and/or vehicle is preincubated with 50 U/ml enzyme‡ for 15 minutes at 37°C in modified Tris-HCl buffer pH 7.2. The reaction is initiated by addition of 10 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:
10 µM DiFMUP
Incubation:
30 min at 37°C
Control Inhibitor:
(NH₄)₆Mo₇O₂₄
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
Adverse / Beneficial Action:
Inhibition of calcineurin, PP2B, may be immunosuppressant, improve allograft survival in solid organ transplantation, as well as useful in the treatment of some inflammatory diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
DrugMatrixScreen LeadHunter Panel - TW
Item: PP89
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