Products from BPS Bioscience require a minimum order value above 400€Application: 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 dynamicregulation of cAMP and cGMP signaling. PDE10A is a dual substrate PDE highlyexpressed in striatal medium spiny neurons. PDE10A inhibitors can improve thecognitive symptoms of schizophrenia, and exhibit potential therapeutic value forHuntington's Disease. 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 PDE10A2 Assay Kit is a fluorescence polarization (FP), homogeneous, 96-well assay kit designed for the screening and profiling of PDE10A2 (Phosphodiesterase 10A2) inhibitors. This assay takes advantage of a specific fluorescent phosphate-binding nanoparticle. The kit contains enough purified recombinant PDE10A2, fluorescent probe, PDE assay buffer, Binding Agent, and diluent for 100 reactions. The assay uses a fluorescein-labeled cyclic adenosine monophosphate (cAMP-FAM for PDE10A2), in which the phosphate group is engaged within the cyclic nucleotide. This is a very small molecule that rotates fast (low FP). PDE10A2 catalyzes the hydrolysis of the phosphodiester bond in the cyclic nucleotide and frees the phosphate group. In a second step the free phosphate group is recognized by a specific phosphate-binding nanobead (Binding Agent) leading to the formation of a large complex, with restricted movement (high FP). FP is proportional to PDE10A2 activity.
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 PDE10A inhibitor screening assay kit comes in a convenient 96-well format, with purified PDE10A enzyme, fluorescently labeled PDE10A substrate (cAMP), binding agent, and PDE assay buffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Threlfell S, Sammut S, Menniti FS, Schmidt CJ, West AR. J Pharmacol Exp Ther 2009; 328(3):785-95.
2. Menniti FS, Chappie TA, Humphrey JM, Schmidt CJ. Curr Opin Investig Drugs 2007; 8(1):54-9. Application Reference(s):
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility (2014)
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