Supplier: BPS Bioscience
Cat no.: 60350
Amount: 96 reactions
Applications: Useful for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Storage/Stability: At least 6 months from date of receipt, when stored as directed. Kit components require different storage conditions. Be sure to store each component at the proper temperature upon arrival.
Supplied As: The PDE5A1 inhibitor screening assay kit comes in a convenient 96-well format, with purified PDE5A1 enzyme, fluorescently labeled PDE5 substrate (cGMP), binding agent, and PDE assay buffer for 100 enzyme reactions.
Phosphodiesterases (PDEs) play an important role in dynamic regulation of cAMP and cGMP signaling. PDE5A1, also known as cGMP-inhibited phosphodiesterase, has been implicated in cardiovascular function and fertility. The PDE5A1 Assay Kit is designed for identification of PDE5A1 inhibitors using fluorescence polarization. The assay is based on the binding of a fluorescent nucleotide monophosphate generated by PDE5A1 to the binding agent.
Phosphodiesterases catalyze the hydrolysis of the phosphodiester bond in dye-labeled cyclic monophosphates. Beads selectively bind the phosphate group in the nucleotide product. This increases the size of the nucleotide relative to unreacted cyclic monophosphate. In the polarization assay, dye molecules with absorption transition vectors parallel to the linearly-polarized excitation light are selectively excited. Dyes attached to the rapidly-rotating cyclic monophosphates will obtain random orientations and emit light with low polarization. Dyes attached to the slowly-rotating nucleotide-bead complexes will not have time to reorient and therefore will emit highly polarized light.
Product information: PDE5A1 Assay Kit (bpsbioscience.com)