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Applications: Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Background: Phosphodiesterases (PDEs) play an important role in the dynamic regulation of cAMP and cGMP signaling. PDE9A is primarily expressed in spleen, smallintestine, and brain. PDE9 inhibitors have been studied as therapeutics for treatment ofcardiovascular diseases, diabetes, and neurodegenerative disorders. Phosphodiesterases catalyze the hydrolysis of the phosphodiester bond in dye-labeledcyclic monophosphates. Beads selectively bind the phosphate group in the nucleotideproduct. This increases the size of the nucleotide relative to unreacted cyclicmonophosphate. In the polarization assay, dye molecules with absorption transitionvectors parallel to the linearly-polarized excitation light are selectively excited. Dyesattached to the rapidly-rotating cyclic monophosphates will obtain random orientationsand emit light with low polarization. Dyes attached to the slowly-rotating nucleotide-beadcomplexes will not have time to reorient and therefore will emit highly polarized light.
Contraindications: DMSO >1%, strong acids or bases, ionic detergents, high salt
Description: The PDE9AAssay Kit is designed for identification of PDE9A inhibitors using fluorescencepolarization. The assay is based on the binding of a fluorescent nucleotidemonophosphate generated by PDE9A to the binding agent. The key to the PDE9A Assay Kit is thespecific binding agent. Using this kit, only two simple steps on a microtiter plate arerequired for PDE9A reactions. First, the fluorescently labeled cGMP is incubated with asample containing PDE9A for 1 hour. Second, a binding agent is added to the reactionmix to produce a change in fluorescent polarization that can then be measured using afluorescence reader.
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 PDE9A inhibitor screening assay kit comes in a convenient 96-well format, includingpurified PDE9A enzyme, fluorescently labeled PDE9 substrate (cGMP), binding agent,and PDE assay buffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: Wang, H. et al. (2010) J. Med Chem. 53 (4): 1726-31.
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