Phosphodiesterase (PDE) Assay Services

Phosphodiesterases (PDEs) catalyze the hydrolysis of cyclic AMP and cyclic GMP. Inhibition of PDEs prevents the regulation of these second messengers and was found useful in the treatment of a variety of conditions including pulmonary hypertension, acute refractory cardiac failure, erectile dysfunction, etc.

  • The activity of PDEs is measured with the Transcreener AMP2/GMP2 FP PDE assay platform (BellBrook labs)
  • Low and large scale screening, as well as high-throughput screening options, are available
  • Custom-tailored assay development possible
  • All phosphodiesterases are produced in house and available for purchase. 

List of Targets

Target Synonyms Data
PDE1A Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Data sheet
PDE1B Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B Data sheet
PDE1C Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C Data sheet
PDE2A cGMP-dependent 3',5'-cyclic phosphodiesterase Data sheet
PDE3A cGMP-inhibited 3',5'-cyclic phosphodiesterase A Data sheet
PDE3B cGMP-inhibited 3',5'-cyclic phosphodiesterase B Data sheet
PDE4A cAMP-specific 3',5'-cyclic phosphodiesterase 4A Data sheet
PDE4B cAMP-specific 3',5'-cyclic phosphodiesterase 4B Data sheet
PDE4C cAMP-specific 3',5'-cyclic phosphodiesterase 4C Data sheet
PDE4D cAMP-specific 3',5'-cyclic phosphodiesterase 4D Data sheet
PDE5A cGMP-specific 3',5'-cyclic phosphodiesterase Data sheet
PDE7A High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A Data sheet
PDE8A High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A Data sheet
PDE9A High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A Data sheet
PDE10A cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Data sheet

Assay Details

Assay Format

Assay principle for compound screening against phosphodiesterases based on quantification of a fluorescent tracer with the transcreener AMP2/GMP2 kit

 

PDE converts cAMP or cGMP to AMP or GMP which displace a fluorescent tracer from an antibody selective for AMP and GMP resulting in a reduction of the fluorescence polarization signal.

Assay Setup

Setups: Single-dose screening in duplicates or IC50 value determination with 5 or 10 concentrations. Other screening formats are available upon request.

Controls: No inhibitor (DMSO vehicle) control and for every assay, one target-specific control compound is tested in 10-dose IC50 format. 

Turnaround time: 10 business days for standard projects. Expedited scheduling and data delivery can be arranged prior to the commencement of the studies.

Report: The raw data, % enzyme activity and control compound IC50 values will be reported in Excel format for single-dose assays. For IC50 orders, raw data, IC50 values, and curve fitting will be delivered in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.

Screening facility: This assay is performed at our screening facility in Malvern, PA, US.

Compound requirements: In brief, for a standard project, 20 µl of a 10 mM DMSO stock or solid material is needed. Less material is needed for large scale screening. Please refer to our FAQs for information regarding compound preparation and shipping.