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

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15136:

The LanthaScreen® TR-FRET TR (thyroid receptor) alpha Coactivator Assay Kit provides a sensitive and robust method for highthroughput screening of potential TR 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 TR alpha ligand-binding domain (TR alpha-LBD) that is tagged with glutathione-S-transferase (GST) in a homogeneous, mix-and-read assay format.

To Assay:
When performing the LanthaScreen® TR-FRET TR alpha coactivator assay, TR alpha-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb anti-GST antibody. After an incubation period at room temperature, the 520 nm/495 nm TR-FRET ratio is calculated and used to determine the EC50 from a dose response curve of the compound. Based on the biology of the TR alpha-coactivator peptide interaction, the ligand EC50 is a composite value representing the amount of ligand required to bind to receptor, induce a conformational change, and recruit coactivator peptide (Figure 1).

Contents and Storage:
The LanthaScreen® TR-FRET TR alpha Coactivator Assay Kit contains TR alpha-LBD (GST) protein, fluorescently labeled SRC2-2 coactivator peptide, Tb-labeled anti-GST antibody, and buffers. Store components as indicated in the assay protocol (-80°C, -20°C, or +4°C).

PolarScreen™ Androgen Receptor Competitor Assay Kit, Red

The PolarScreen™ Androgen Receptor Competitor Assay Kit, Red, provides a sensitive and efficient method for high-throughput, fluorescence polarization-based screening of potential androgen receptor (AR) ligands. The kit uses insect cell-expressed rat AR ligand binding domain tagged with glutathione-S-transferase (GST) and histidine (also available separately), plus a novel, high-affinity, fluorescent androgen receptor ligand (Fluormone AL 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 Androgen Receptor Competitor Assay is:

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

How the Assay Works
The kit uses the rat AR ligand-binding domain tagged with His and GST [AR-LBD(His-GST)]. AR-LBD(His-GST) is added to a fluorescently-tagged androgen ligand (FluormoneAL Red) in the presence of competitor test compounds in microwell plates. Competitors displace the fluorescent FluormoneAL Red Ligand from the AR-LBD/FluormoneAL Red complex, causing the fluorescent ligand to tumble rapidly during its fluorescence lifetime, resulting in a low polarization value. Noncompetitors will not displace the fluorescent ligand from the complex; therefore, the polarization value remains high. The shift in polarization value in the presence of the test compounds is used to determine relative affinity of test compounds for the AR-LBD.

Contact us for bulk quantities or for assistance with other nuclear receptor assay needs, from assay development to library screening and beyond.

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

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15137:

The LanthaScreen® TR-FRET RAR (retinoic acid receptor) beta Coactivator Assay Kit provides a sensitive and robust method for highthroughput screening of potential RAR beta 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 RAR beta ligand-binding domain (RAR beta-LBD) that is tagged with glutathione-S-transferase (GST) in a homogeneous, mix-and-read assay format.

When running the LanthaScreen® TR-FRET RAR beta coactivator assay in agonist mode to identify agonist compounds, RAR 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 RAR 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 recruit coactivator peptide (Figure 1).

Contents and Storage:
The LanthaScreen® TR-FRET RAR beta Coactivator Assay Kit contains RAR beta-LBD (GST) protein, fluorescently labeled SRC2-2 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 PPAR gamma Coactivator Assay Kit, goat

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15126:

The LanthaScreen® TR-FRET PPAR gamma Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential PPAR gamma 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 Peroxisome Proliferator Activated Receptor (PPAR) gamma ligand-binding domain (PPAR gamma-LBD) that is tagged with glutathione-S-transferase (GST), in a homogenous mix-and-read assay format.

Agonist mode
To run the LanthaScreen® TR-FRET Peroxisome Proliferator Activated gamma Receptor Coactivator Assay in agonist mode (to identify agonist compounds), PPAR gamma-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-anti-GST antibody. After an incubation period at room temperature, the TR-FRET 520:495 emission ratio is calculated and used to determine the EC50 from a dose response curve of the compound. Based on the biology of the PPAR gamma-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).

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

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

PolarScreen™ ER Alpha Competitor Assay, Green

The PolarScreen™ ER (Estrogen Receptor) Alpha Competitor Assay Kit, Green, provides a sensitive and efficient method for high-throughput, fluorescence polarization-based screening of potential ER alpha ligands. The kit uses insect cell-expressed, full-length, native (untagged) human estrogen receptor alpha (available separately, Cat. No. A15674) and a novel, high-affinity, fluorescent estrogen ligand (Fluormone ES2 Green) in a homogenous, mix-and-read assay format.

This kit produces a green color read-out; a "red" 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 drugdiscoverytech@lifetech.com.

PolarScreen™ ER Alpha Competitor Assay, Green, is:

• Complete & ready-to-use out of the box—all reagents included, just add your test compounds
• High throughput compatible—800 x 20 µL fluorescence polarization assays in a 384-well plate
• Convenient—available in bulk sizes for larger screening needs

How the Assay Works
Full length ER alpha is added to a fluorescent estrogen ligand to form an ER-Fluormone ES2 complex. This complex is added to individual test compounds in multiwell plates. To determine relative affinity, the assay measures fluorescence polarization. Competing test compounds will displace the Fluormone ES2 ligand from ER alpha, permitting it to tumble rapidly and resulting in low polarization values. A shift in the fluorescence polarization value in the presence of test compound is used to determine the relative affinity of test compounds for ER alpha.

All components are manufactured under the strictest quality parameters. This product's performance, per the Certificate of Analysis, is guaranteed for 6 months after purchase. Contact us for bulk quantities or for assistance with other nuclear receptor assay needs, from assay development to library screening and beyond.

LanthaScreen™ TR-FRET ER alpha Coactivator Assay Kit

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

Agonist Mode
To run the LanthaScreen TR-FRET ER alpha Coactivator Assay in agonist mode (to identify agonist compounds), ER alpha-LBD is added to ligand test compounds, followed by the addition of a mixture of fluorescein-coactivator peptide and Tb-anti-GST antibody. After incubation at room temperature, the TR-FRET 520:495 nm emission ratio is calculated and used to determine the EC50 from a dose response curve of the compound. Based on the biology of the ER 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.

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

LanthaScreen™ TR-FRET Glucocorticoid Receptor Competitive Binding Kit

The LanthaScreen® TR-FRET Glucocorticoid Receptor Competitive Binding Assay Kit provides a sensitive and robust method for high-throughput screening (HTS) of ligands for glucocorticoid receptor (GR). The kit uses a human GR ligand-binding domain (GR-LBD) tagged with glutathione S-transferase (GST) (also available separately), a terbium-labeled anti-GST antibody, and a fluorescent small-molecule GR ligand (Fluormone™ GS1) in a homogeneous mix-and-read assay format.

The Lanthascreen Gluococorticoid Receptor 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 ER beta Coactivator Assay Kit

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

Agonist Mode
To run the LanthaScreen TR-FRET ER beta Coactivator Assay in agonist mode (to identify agonist compounds), ER beta-LBD is added to ligand test compounds followed by the addition of a mixture of fluorescein-coactivator peptide and Tb-anti-GST antibody. After room temperature incubation, the TR-FRET 520:495 emission ratio is calculated and used to determine the EC50 from a dose response curve of the compound. Based upon the biology of the ER 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 recruit coactivator peptide.

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

LanthaScreen™ TR-FRET Androgen Receptor Coactivator Assay Kit

The LanthaScreen® TR-FRET Androgen Receptor Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential androgen receptor (AR) ligands as agonists of coactivator recruitment or antagonists of agonist-dependent coactivator recruitment. In both the agonist and antagonist modes, the homogeneous mix-and-read assay uses a rat AR ligand-binding domain (AR-LBD) tagged with hexahistidine and glutathione-S-transferase (GST) (also available separately), a terbium (Tb)-labeled anti-GST antibody, and a fluorescein-labeled coactivator peptide.

Agonist Mode
When the LanthaScreen TR-FRET Androgen Receptor Coactivator Assay is run in agonist mode (to identify agonist compounds), AR-LBD is added to ligand test compounds, followed by the addition of a mixture of fluorescein-coactivator peptide and Tb-anti-GST antibody. After room temperature incubation, the TR-FRET 520:495 nm emission ratio is calculated and used to determine the EC50 from a dose response curve of the compound. 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 Androgen Receptor Coactivator Assay is run in antagonist mode (to identify antagonist compounds), AR-LBD is added to ligand test compounds, followed by addition of a mixture of DHT agonist, fluorescein-coactivator peptide, and Tb-anti-GST antibody. The concentration of DHT agonist used in this mode is the EC80 concentration as determined by first running the assay in agonist mode. An example of data produced in the antagonist mode is shown in the figure below.

LanthaScreen™ TR-FRET PXR (SXR) Competitive Binding Assay Kit, goat

This kit contains Goat Tb-Anti-GST antibody; other kit components are the same as kit A15142:

The LanthaScreen® TR-FRET PXR (SXR) Competitive Binding Assay Kit provides a sensitive and robust method for high-throughput screening (HTS) of ligands for the pregnane X receptor (PXR), also known as the steroid and xenobiotic receptor (SXR). The kit uses a terbium (Tb)-labeled anti-GST antibody, a fluorescent small-molecule PXR ligand (Fluormone™ PXR (SXR) Green), and a human PXR (SXR) ligand-binding domain that is tagged with glutathione S-transferase (GST) in a homogeneous mix-and-read assay format.

To assay:
When running the LanthaScreen® TR-FRET PXR (SXR) competitive binding assay, a Tb-labeled anti-GST antibody is used to indirectly label the receptor by binding to its GST tag. Competitive ligand binding is detected by a test compound’s ability to displace a fluorescent ligand (tracer) from the receptor, which results in a loss of FRET signal between the Tb-anti-GST antibody and the tracer (Figure 1). This type of binding assay is analogous to radioligand-based assays, except that it eliminates handling of radioactivity and enables a homogeneous, “addition-only " format.

PolarScreen™ ER Beta Competitor Assay Kit, Green

The PolarScreen™ ER Beta Competitor Assay Kit, Green, provides a sensitive and efficient method for high-throughput, fluorescence polarization-based screening of potential estrogen receptor (ER) beta ligands. The kit uses insect cell-expressed, full-length, native (untagged) human ER beta (A15664) and a novel, high-affinity, fluorescent estrogen ligand (Fluormone™ ES2) in a homogenous, mix-and-read assay format.

This kit produces a green color read-out; a "red" kit is also available (A15891). 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 email drugdiscoverytech@lifetech.com.

The PolarScreen™ ER Beta Competitor Assay Kit is:

• Complete & ready-to-use out of the box—all reagents included, just add your test compounds
• High throughput compatible—20 µL fluorescence polarization assays in a 384-well plate
• Convenient—available in bulk sizes for larger screening needs

How the Assay Works
Full-length ER beta is added to a fluorescent estrogen ligand to form an ER-Fluormone™ ES2 complex. This complex is added to individual test compounds in multiwell plates. To determine relative affinity, the assay measures fluorescence polarization. Competing test compounds will displace the Fluormone™ ES2 ligand from ER beta, permitting it to tumble rapidly and resulting in low polarization values. A shift in the fluorescence polarization value in the presence of test compound is used to determine the relative affinity of test compounds for ER beta.

All components are manufactured under the strictest quality parameters. This product's performance, per the Certificate of Analysis, is guaranteed for 6 months after purchase. Contact us for bulk quantities or for assistance with other nuclear receptor assay needs, from assay development to library screening and beyond.

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 Progesterone Receptor Coactivator Assay Kit

The LanthaScreen® TR-FRET Progesterone Receptor Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential progesterone receptor (PR) ligands as agonists or antagonists of ligand-dependent coactivator recruitment. The kit uses a PR ligand--binding domain (PR-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 homogenous mix-and-read assay format.

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

LanthaScreen™ TR-FRET PPAR gamma Coactivator Assay Kit, rabbit

This kit contains Rabbit Tb-Anti-GST antibody; other kit components are the same as kit PV4548:

The LanthaScreen® TR-FRET PPAR gamma Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential PPAR gamma 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 Peroxisome Proliferator Activated Receptor (PPAR) gamma ligand-binding domain (PPAR gamma-LBD) that is tagged with glutathione-S-transferase (GST), in a homogenous mix-and-read assay format.

Agonist mode
To run the LanthaScreen® TR-FRET Peroxisome Proliferator Activated gamma Receptor Coactivator Assay in agonist mode (to identify agonist compounds), PPAR gamma-LBD is added to ligand test compounds followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-anti-GST antibody. After an incubation period at room temperature, the TR-FRET 520:495 emission ratio is calculated and used to determine the EC50 from a dose response curve of the compound. Based on the biology of the PPAR gamma-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).

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

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

PolarScreen™ Progesterone Receptor Competitor Assay Kit, Red

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:

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

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.