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PDE4B2 Assay Kit
PDE4B2 Assay Kit
Artikelnummer
BPS60343
Verpackungseinheit
96 rxns.
Hersteller
BPS Bioscience
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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. PDE4 selective inhibitors are currently in clinical trials for thetreatment of diseases related to inflammatory disorders. Increased expression of PDE4B2was observed in the near-term myometrium. PDE4B2 can be induced by its own substrate,under the control of one of the major utero-contractile agonist, PGE2. 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 PDE4B2 AssayKit is designed for identification of inhibitors of PDE4B2 using fluorescence polarization. Theassay is based on the binding of a fluorescent nucleotide monophosphate generated byPDE4B2 to the binding agent. The key to the PDE4B2 Assay Kit is the specific bindingagent. Using this kit, only two simple steps on a microtiter plate are required for PDE4B2reactions. First, the fluorescently labeled cAMP is incubated with a sample containingPDE4B2 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 PDE4B2 Assay Kit comes in a convenient 96-well format, with purified PDE4B2enzyme, fluorescently labeled PDE4B2 substrate (cAMP), binding agent, and PDE assaybuffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Cullen MD, et al. Bioorg Med Chem Lett. 2008; 18(4):1530-3.
2. Méhats C, et al. BMC Pregnancy Childbirth. 2007; 7 Suppl 1:S12.Application Reference(s):
Structure based virtual screening to identify selective phosphodiesterase 4B inhibitors (2015)
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. PDE4 selective inhibitors are currently in clinical trials for thetreatment of diseases related to inflammatory disorders. Increased expression of PDE4B2was observed in the near-term myometrium. PDE4B2 can be induced by its own substrate,under the control of one of the major utero-contractile agonist, PGE2. 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 PDE4B2 AssayKit is designed for identification of inhibitors of PDE4B2 using fluorescence polarization. Theassay is based on the binding of a fluorescent nucleotide monophosphate generated byPDE4B2 to the binding agent. The key to the PDE4B2 Assay Kit is the specific bindingagent. Using this kit, only two simple steps on a microtiter plate are required for PDE4B2reactions. First, the fluorescently labeled cAMP is incubated with a sample containingPDE4B2 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 PDE4B2 Assay Kit comes in a convenient 96-well format, with purified PDE4B2enzyme, fluorescently labeled PDE4B2 substrate (cAMP), binding agent, and PDE assaybuffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Cullen MD, et al. Bioorg Med Chem Lett. 2008; 18(4):1530-3.
2. Méhats C, et al. BMC Pregnancy Childbirth. 2007; 7 Suppl 1:S12.Application Reference(s):
Structure based virtual screening to identify selective phosphodiesterase 4B inhibitors (2015)
| Artikelnummer | BPS60343 |
|---|---|
| Hersteller | BPS Bioscience |
| Hersteller Artikelnummer | 60343 |
| Green Labware | Nein |
| Verpackungseinheit | 96 rxns. |
| Mengeneinheit | PAK |
| Produktinformation (PDF) | Download |
| MSDS (PDF) |
|
Immer für Sie da
Gernot Ensinger, M.Sc.
Laurent Haze
