Products from BPS Bioscience require a minimum order value above 400€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. PDE4D is a regulator of airway smooth-muscle contractility, andhas been identified as a potential risk predictor for ischemic stroke. Additionally, PDE4D hasbeen associated with asthma pathophysiology and bone formation. The PDE4D geneencodes at least 9 different isoforms.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 PDE4D2 Assay Kit is designed for identification ofinhibitors of PDE4D2 using fluorescence polarization. The assay is based on the binding ofa fluorescent nucleotide monophosphate generated by PDE4D2 to the binding agent. The key to the PDE4D2 Assay Kit is the specific bindingagent. Using this kit, only two simple steps on a microtiter plate are required for PDE4D2reactions. First, the fluorescently labeled cAMP is incubated with a sample containingPDE4D2 for 1 hour. Second, a binding agent is added to the reaction mix to produce achange in fluorescent polarization that can then be measured using a fluorescence readerequipped for the measurement of fluorescence polarization.
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 PDE4D2 Assay Kit comes in a convenient 96-well format, with purified PDE4D2enzyme, fluorescently labeled PDE4D substrate (cAMP), binding agent, and PDE assaybuffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: Chandrasekaran A, et al., Cell Signal. 2008;20(1):139-53.Application Reference(s):
1.
Structure based virtual screening to identify selective phosphodiesterase 4B inhibitors (2015)
2. Active components of ginger potentiate β-agonist-induced relaxation of airway smooth muscle by modulating cytoskeletal regulatory proteins (2014)
3. Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4 (2013)
4. Quercetin acutely relaxes airway smooth muscle and potentiates β-agonist-induced relaxation via dual phosphodiesterase inhibition of PLCβ and PDE4 (2013)
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