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The PolarScreen™ Progesterone Receptor Competitor Assay Kit, Red, provides a sensitive and efficient method for high-throughput, fluorescence polarization-based screening of potential progesterone receptor (PR) ligands. The kit uses insect cell-expressed, human progesterone receptor ligand binding domain tagged with glutathione-S-transferase (GST) (also available separately) and a novel, high-affinity, fluorescent progesterone ligand (Fluormone™ PL Red) in a homogenous, mix-and-read assay format.
This kit produces a red color read-out; a 'green' kit is also available. Both kits suitably determine the IC50s of competitive compounds. Color choice depends on the spectral properties of the compounds to be screened and the available instrumentation. For additional information or assistance contact us at drugdiscoverytech@lifetech.com.
The PolarScreen Progesterone Receptor Competitor Assay is:
How the Assay Works
An N-terminal fusion of glutathione transferase to the ligand-binding domain of the human progesterone receptor (PR-LBD(GST)) is added to a fluorescently-tagged progesterone ligand (Fluormone PL Red) in the presence of competitor test compounds in microwell plates. The presence of effective competitors prevents the formation of a PL Red/PR-LBD(GST) complex resulting in a decrease of the polarization value. The shift in polarization value in the presence of test compounds is used to determine relative affinity of test compounds for PR-LBD(GST).
Contact us for bulk quantities or for assistance with other nuclear receptor assay needs, from assay development to library screening and beyond.