PDE10A1 TR-FRET Assay Kit

Catalog # 60709
Size: 96 reactions

DESCRIPTION: 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 cytosol, whereas PDE10A2 is a
membrane-associated protein.
The PDE10A1 TR-FRET Assay Kit is designed for identification of inhibitors of PDE10A1
using TR-FRET (Time Resolved Fluorescence Resonance Energy Transfer) technology.
The assay is based on the generation of FAM-labeled nucleotide monophosphates by
the phosphodiesterase. These phosphate groups bind to terbium-labeled nanoparticles,
resulting in energy transfer from the terbium to the FAM, which emits a fluorescent signal
at 520 nm. The change in fluorescent intensity can be easily measured using a
fluorescence plate reader.

The PDE10A1 TR-FRET Assay Kit comes in a convenient 96-well format, with purified
PDE10A1 enzyme, fluorescently labeled PDE substrate (cAMP), binding agent, and
PDE assay buffer for 100 enzyme reactions. Using this kit, only two simple steps on a
microtiter plate are required for the PDE10A1 activity assay. First, the fluorescentlabeled
cAMP is incubated with a sample containing PDE10A1 for 1 hour. Second, a
binding agent and a terbium donor are added to the reaction mix and incubated for 1
hour. Then, fluorescence intensity can be measured using a fluorescence reader.

APPLICATIONS: Great for screening small molecular inhibitors for drug discovery and
HTS applications.

STABILITY: 6 months from date of receipt when stored as directed.

COMPONENTS:

REFERENCE(S):
1) Akinori Nishi and Gretchen L. Snyder. J Pharmacol Sci., 2010, 114: 6 – 16.
2) Kenji Omori and Jun Kotera. Circulation Research. 2007; 100: 309-327.

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