The PDE10A1 Assay Kit is designed for identification of PDE10A1 inhibitors using fluorescence polarization. The assay is based on the binding of a fluorescent nucleotide monophosphate generated by PDE10A1 to the binding agent. The key to the PDE10A1 Assay Kit is the specific binding agent. Using this kit, only two simple steps on a microtiter plate are required for PDE10A1 reactions. First, the fluorescently labeled cAMP is incubated with a sample containing PDE10A1 for 1 hour. Second, a binding agent is added to the reaction mix to produce a change in fluorescent polarization. The FP signal is measured using a fluorescent microplate reader capable of measuring fluorescence polarization.
The PDE10A1 inhibitor screening assay kit comes in a convenient 384-well format, including purified PDE10A1 enzyme, fluorescently labeled PDE10A1 substrate (cAMP), binding agent, and PDE assay buffer for 400 enzyme reactions.
Format
COMPONENTS:
UniProt #
Q9Y233
Background
Phosphodiesterases (PDEs) play an important role in dynamic regulation of
cAMP and cGMP signaling. PDE10A is a dual substrate PDE highly expressed in striatal
medium spiny neurons. PDE10A inhibitors can improve the cognitive symptoms of
schizophrenia, and exhibit potential therapeutic value for Huntington’s disease. PDE10A1 is
located in the cytosol, whereas PDE10A2 is a membrane-associated protein.
References
1) Nishi, A., and Snyder, G.L. J. Pharmacol. Sci., 2010, 114: 6-16.
2) Omori, K., and Kotera, J. Circulation Res. 2007; 100: 309-327.
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.
Instructions for Use
See assay kit data sheet for detailed protocol.
Applications
Useful for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Shipping Temperature
-80°C (dry ice)
Notes
MATERIALS OR INSTRUMENTS REQUIRED BUT NOT SUPPLIED:
Fluorescent microplate reader capable to measure fluorescence polarization
Warnings
This assay requires a fluorescent microplate reader capable of measuring fluorescence polarization (FP) and equipped with the required partsto read the FP signal. For more information FP technology, visit our Tech Note: FP, assay principles and applications.
Avoid freeze/thaw cycles.
Disclaimers and Limitations
BPS Bioscience assay kits are validated using the listed components according to our specific protocol. Any deviations to kit components or protocols, such as using different proteins, cell/tissue lysates, or buffers (including using the same component from other commercial sources) will void any warranties on the performance of the assay kit and is not recommended.
End-users should immediately report any issues to [email protected] upon receipt of the kit, such as missing components, damaged vials, no dry ice, etc.
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