Biochemical Nuclear Receptor Assays - Kits

LanthaScreen™ TR-FRET PPAR delta Coactivator Assay Kit, goat

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15134:

The LanthaScreen® TR-FRET PPAR (peroxisome proliferator activated receptor) delta Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential PPAR delta ligands as agonists of ligand-dependent coactivator recruitment. The kit uses a terbium (Tb)-labeled anti-GST antibody, a fluorescein-labeled coactivator peptide, and a human recombinant PPAR delta ligand-binding domain (PPAR delta-LBD) that is tagged with glutathione-S-transferase (GST), in a homogeneous mix-and-read assay format.

When running the LanthaScreen® TR-FRET PPAR delta Coactivator Assay in agonist mode (to identify agonist compounds), PPAR delta-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-labeled coactivator peptide and Tb-labeled anti-GST antibody. After an incubation period at room temperature, the TR-FRET ratio of 520/495 is calculated and can be used to determine the EC50 from a dose response curve of the compound. Based on the biology of the PPAR delta-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 1).

Contents and Storage:
The LanthaScreen® TR-FRET PPAR delta Coactivator Assay Kit contains PPAR delta-LBD (GST) protein, fluorescently labeled C33 coactivator peptide, Tb-anti-GST antibody, and buffers. Store components as indicated in the assay protocol (-80°C, -20°C or 4°C).

LanthaScreen™ TR-FRET LXR alpha Coactivator Assay Kit, rabbit

This kit contains Rabbit Tb-Anti-GST antibody; other kit components are the same as kit PV4655:

The LanthaScreen® TR-FRET LXR (liver X receptor) alpha Coactivator Assay provides a sensitive and robust method for high-throughput screening of potential LXR alpha ligands as agonists of coactivator recruitment. The kit uses a terbium (Tb)-labeled anti-GST antibody, a fluorescein-labeled coactivator peptide, and an LXR alpha ligand-binding domain (LBD) that is tagged with glutathione-S-transferase (GST), in a homogeneous mix-and-read assay format.

In the LanthaScreen® TR-FRET LXR alpha Coactivator Assay, LXR alpha-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-labeled anti-GST antibody. After an incubation period at room temperature, the 520 nm/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 LXR alpha-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 (Figure 1).

Contents and Storage:
The LanthaScreen® TR-FRET LXR alpha Coactivator Assay Kit contains LXR alpha-LBD (GST) protein, fluorescently labeled TRAP220/DRIP-2 coactivator peptide, Tb-labeled anti-GST antibody, and buffers. Store components as indicated in the assay protocol (-80°C, -20°C, or +4°C).

LanthaScreen™ TR-FRET ERR beta Coactivator Assay Kit, goat

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15139:

The LanthaScreen® TR-FRET ERR (estrogen related receptor) beta Coactivator Assay Kit provides a sensitive and robust method for highthroughput screening of potential ERR beta ligands as inverse agonists of ligand-dependent coactivator displacement. The kit uses a terbium (Tb)-labeled anti-GST antibody, a fluorescein-labeled coactivator peptide, and a human recombinant ERR beta ligand-binding domain (ERR beta-LBD) that is tagged with glutathione-S-transferase (GST) in a homogeneous mix-and-read assay format.

To assay:

When running the LanthaScreen® ERR beta TR-FRET Coactivator Assay, ERR beta-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-labeled anti-GST antibody. After an incubation period at room temperature, the 520 nm/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 ERR beta-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 displace coactivator peptide (see Figure 1).

LanthaScreen™ TR-FRET PPAR alpha Coactivator Assay Kit, goat

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15133:

The LanthaScreen® TR-FRET PPAR (peroxisome proliferator activated receptor) alpha Coactivator Assay provides a sensitive and robust method for high-throughput screening of potential PPAR alpha ligands as agonists or antagonists of ligand-dependent coactivator recruitment. The kit uses a terbium (Tb)-labeled anti-GST antibody, a fluorescein-labeled coactivator peptide, and a human recombinant PPAR alpha ligand-binding domain (PPAR alpha-LBD) that is tagged with glutathione-S-transferase (GST) in a homogeneous mix-and-read assay format.

Agonist mode:
When running the LanthaScreen® TR-FRET PPAR alpha Coactivator Assay in agonist mode (to identify agonist compounds), PPAR alpha- LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-labeled anti-GST antibody. After an incubation period at room temperature, the 520 nm/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 PPAR alpha-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 1).

Antagonist mode:
When the LanthaScreen® TR-FRET PPAR alpha Coactivator Assay is run in antagonist mode (to identify antagonist compounds), PPAR alpha-LBD is added to ligand test compounds followed by addition of a mixture of agonist, fluorescein-coactivator peptide, and Tb-labeled anti-GST antibody (Figure 2). The concentration of agonist used in this mode is the EC80 concentration as determined by first running the assay in agonist mode.

Contents and Storage:
The LanthaScreen® TR-FRET PPAR alpha Coactivator Assay Kit contains PPAR alpha-LBD (GST) protein, fluorescently labeled PGC1a coactivator peptide, Tb-labeled anti-GST antibody, and buffers. Store components as indicated in the assay protocol (-80°C, -20°C, or 4°C).

LanthaScreen™ TR-FRET ER alpha Competitive Binding Kit

The LanthaScreen® TR-FRET ER alpha Competitive Binding Kit provides a sensitive and robust method for high-throughput screening (HTS) of ligands for estrogen receptor (ER) alpha. The kit uses a human ER alpha ligand-binding domain (LBD) that is tagged with glutathione S-transferase (GST), a terbium-labeled anti-GST antibody, and a fluorescent small-molecule ER ligand (Fluormone™ ES2) in a homogeneous mix-and-read assay format.

The Lanthascreen ER alpha Competitive Binding Assay is:

• Complete & ready-to-use out of the box—all reagents included, just add your test compounds
• High throughput compatible—TR-FRET assays in a 384-well plate
• Convenient—components available in bulk sizes for larger screening needs

LanthaScreen™ TR-FRET RXR alpha Coactivator Assay Kit, goat

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15138:

The LanthaScreen® TR-FRET Retinoid X Receptor alpha Coactivator Assay provides a sensitive and robust method for high-throughput screening of potential RXR alpha ligands as agonists of ligand-dependent coactivator recruitment. The kit uses a terbium (Tb)-labeled anti- GST antibody, a fluorescein-labeled coactivator peptide, and a human recombinant RXR alpha ligand-binding domain (RXR alpha-LBD) that is tagged with glutathione-S-transferase (GST) in a homogeneous mix-and-read assay format.

To assay:
When running the LanthaScreen® TR-FRET Retinoid X Receptor alpha Coactivator Assay in agonist mode (to identify agonist compounds), RXR alpha-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-labeled anti-GST antibody. After an incubation period at room temperature, the TR-FRET ratio of 520/495 is calculated and can be used to determine the EC50 from a dose-response curve of the compound. Based on the biology of the RXR alpha-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 1).