LanthaScreen™ TR-FRET Glucocorticoid Receptor Coactivator Assay Kit

Catalog number: A15899

LanthaScreen™ TR-FRET Glucocorticoid Receptor Coactivator Assay Kit

Catalog number: A15899
Catalog Number
A15899
Unit Size
800 x 20 µL assays
Price (USD)
Price: 1,752.00
Your Price:
Availability
-
Quantity
Catalog NumberUnit SizePrice (USD)AvailabilityQuantity
A15899800 x 20 µL assays
Price: 1,752.00
Your Price:
-
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The LanthaScreen® TR-FRET Glucocorticoid Receptor Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential glucocorticoid receptor (GR) ligands as agonists or antagonists of ligand-dependent coactivator recruitment. The kit uses a human recombinant GR ligand-binding domain (GR-LBD) tagged with glutathione-S-transferase (GST) (also available separately), a terbium (Tb)-labeled anti-GST antibody, and a fluorescein-labeled coactivator peptide in a homogeneous mix-and-read assay format.

Agonist Mode
When running the LanthaScreen TR-FRET Glucocorticoid Receptor Coactivator Assay in agonist mode (to identify agonist compounds), GR-LBD is added to ligand test compounds, followed by the addition of a mixture of fluorescein-coactivator peptide and Tb-labeled anti-GST antibody. After incubation at room temperature, the 520/495 nm TR-FRET ratio is calculated and can be used to determine the EC50 from a dose response curve of the compound. Based on the biology of the GR-coactivator peptide interaction, this ligand EC50 is a composite value representing the amount of ligand required to bind to receptor, effect a conformational change, and recruit coactivator peptide (see figure).

Antagonist Mode
When the LanthaScreen TR-FRET Glucocorticoid Receptor Coactivator Assay is run in antagonist mode (to identify antagonist compounds), GR-LBD is added to ligand test compounds followed by the addition of a mixture of agonist, fluorescein-coactivator peptide, and Tb-labeled anti-GST antibody (see figure). The concentration of agonist used in this mode is the EC80 concentration as determined by first running the assay in agonist mode.

Specifications

For Use With (Application)
Co-Factor Interaction Assay, Nuclear Receptor Assay
Product Line
LanthaScreen™

Contents & Storage

1 tube GR Ligand Binding Domain Recombinant Protein (store at -68 to -85°C)
1 tube of Peptide (store at -5 to -30°C)
2 bottles TR-FRET Buffer (store at -5 to -30°C)
1 vial Tb-Anti-GST Ab (store at -5 to -30°C)
1 tube of DTT (store at -5 to -30°C)