Cell-Based Nuclear Receptor Reporter Assays - Kits

GeneBLAzer™ RAR-gamma DA Assay Kit

GeneBLAzer®RAR gamma DA (Division Arrested) cells and RAR gamma-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human retinoic acid receptor gamma (RAR gamma) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-RAR gamma (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both RAR gamma DA cells and RAR gamma-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of all-trans retinoic acid (ATRA). In addition, RAR gamma-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, and stimulation time.

GeneBLAzer™ RXRα-UAS-bla HEK 293T Cells

RXR alpha-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human retinoid X receptor-alpha (RXR alpha) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UASbla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a betalactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-RXR alpha (LBD) fusion protein, the protein binds to the UAS, resulting in expression of alpha-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. RXR alpha-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of 9-cis-retinoic acid. In addition, RXR alpha-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ ERRα-UAS-bla HEK 293T Cells

ERR alpha-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Estrogen related receptor alpha (ERR alpha) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-ERR alpha (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. ERR alpha-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of XCT790, an inverse agonist. In addition, ERR alpha-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ LXR beta DA Assay Kit

GeneBLAzer®LXR beta DA (Division Arrested) cells and LXR beta-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Liver-X receptor-beta (LXR beta) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-LXR beta (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both LXR beta DA cells and LXR beta-UAS-bla HEK 293T 293 cells are functionally validated for Z' and EC50 concentrations of TO901317. In addition, LXR beta-UAS-bla HEK 293T 293 cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ ER Alpha DA Assay Kit

GeneBLAzer®ER alpha DA(Division Arrested) cells and ER alpha-UAS-bla GripTite™ cells contain the ligand-binding domain (LBD) of the human Estrogen receptor alpha (ER alpha) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla GripTite™ cell line. GeneBLAzer®UAS-bla GripTite™ cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-ER alpha (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both ER alpha DA cells and ER alpha-UAS-bla GripTite™cells are functionally validated for Z' and EC50 concentrations of 17-beta Estradiol. In addition, ER alpha-UAS-bla GripTite™cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ AR-UAS-bla Griptite™ Cells

AR-UAS-bla GripTite™ 293 cells contain the ligand-binding domain (LBD) of the rat Androgen receptor (AR) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla GripTite™ 293 cell line. GeneBLAzer®UAS-bla GripTite™ cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-AR (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. AR-UAS-bla GripTite™ 293 cells are functionally validated for Z' and EC50 concentrations of R1881. Cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ ERR Alpha DA Assay Kit

GeneBLAzer®ERR alpha DA(Division Arrested) cells and ERR alpha-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Estrogen related receptor alpha (ERR alpha) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-ERR alpha (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both ERR alpha DA cells and ERR alpha-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of XCT790, an inverse agonist. In addition, ERR alpha-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ PPAR alpha UAS-bla HEK 293T Cellular Assay Kit

The GeneBLAzer® PPAR alpha-UAS-bla HEK 293T Cellular Assay provides an accurate, sensitive, and easy-to-use method for monitoring the cellular response of PPAR alpha to drug candidates or other stimuli.

Features of the The GeneBLAzer® PPAR alpha-UAS-bla HEK 293T Cellular Assay:
Convenience—plate cells and perform assay without additional cell culture steps
Low Noise—the kit uses a Fluorescence Resonance Energy Transfer (FRET)-based ratiometric readout for minimum noise and error
Low Background—the GAL4 fusion prevents any background from endogenous receptor

The Cells
The GeneBLAzer® PPAR alpha-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human peroxisome proliferator-activated receptor alpha (PPAR alpha) fused to the DNA-binding domain of GAL4 transiently transduced (via BacMam virus) into the GeneBLAzer® UAS-bla HEK293T cell line. GeneBLAzer® UAS-bla HEK 293T cells stably express a β-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS).

The Assay
When an agonist binds to the LBD of the GAL4 (DBD)-PPAR alpha (LBD) fusion protein, the protein binds to the UAS, resulting in expression of β-lactamase. The FRET ratiometric readout from the live-cell substrate reduces the absolute and relative errors that can mask the underlying biological response of interest. PPAR alpha UAS-bla HEK 293T cells have been tested for assay performance using variable assay conditions, including cell number, stimulation time, substrate loading time and have been validated for Z′ and EC50 concentrations of GW7647. Additional testing data using alternate stimuli are also available. See the "validation packet" in the documents below to view the data.

Speed and Convenience
Because PPAR alpha UAS-bla HEK 293T cells are transiently transduced with BacMam virus, they are ready to be used in an assay without any additional cell culture steps. Just plate the cells and assay as outlined in the protocol.

Please email our Custom Services team to inquire about obtaining these cells at economical bulk scales.

GeneBLAzer™ FXR-UAS-bla HEK 293T Cells

FXR-UAS-bla HEK 293T 293 cells contain the ligand-binding domain (LBD) of the human farnesoid X receptor (FXR) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UASbla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-FXR (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. FXR-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of chenodeoxycholic acid (CDCA). In addition, FXR-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ TR beta DA Assay Kit

GeneBLAzer®TR beta DA(Division Arrested) cells and TR beta-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Thyroid hormone receptor beta (TR beta) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UASbla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a betalactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-TR beta (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both TR beta DA cells and TR beta-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of T3 Thryoid hormone. In addition, TR beta-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ VDR DA Assay Kit

GeneBLAzer®VDR DA(Division Arrested) cells and VDR-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Vitamin D receptor (VDR) fused to the DNAbinding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-VDR (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both VDR DA cells and VDR-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of Calcitriol (1α, 25-dihydroxyvitamin D3). In addition, VDR-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time.

GeneBLAzer™ PPARδ-UAS-bla HEK 293T Cells

PPAR delta-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Peroxisome Proliferator-Activated Receptor-delta (PPAR delta) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-PPAR delta (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. PPAR delta-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of L-165041. In addition, PPAR delta-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ TR alpha DA Assay Kit

GeneBLAzer®TR alpha DA(Division Arrested) cells and TR alpha-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Thyroid hormone receptor alpha(TR alpha) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla HEK 293T cell line. GeneBLAzer®UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-TR alpha (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both TR alpha DA cells and TR alpha-UASbla HEK 293T 293 cells are functionally validated for Z' and EC50 concentrations of T3 Thryoid hormone. In addition, TR alpha-UAS-bla HEK 293T 293 cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ PPAR delta DA Assay Kit

GeneBLAzer® PPAR delta DA (Division Arrested) cells and PPAR delta-UAS-bla HEK 293T cells contain the ligand-binding domain (LBD) of the human Peroxisome Proliferator-Activated Receptor-delta (PPAR delta) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer® UAS-bla HEK 293T cell line. GeneBLAzer® UAS-bla HEK 293T cells stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-PPAR delta (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both PPAR delta DA cells and PPAR delta-UAS-bla HEK 293T cells are functionally validated for Z' and EC50 concentrations of L-165041. In addition, PPAR delta-UAS-bla HEK 293T cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time (data available upon request). Additional testing data using alternate stimuli are also available.

GeneBLAzer™ ER Beta DA Assay Kit

GeneBLAzer®ER beta DA(Division Arrested) cells and ER beta-UAS-bla GripTite™ 293 cells contain the ligand-binding domain (LBD) of the human Estrogen receptor beta (ER beta) fused to the DNA-binding domain of GAL4 stably integrated in the GeneBLAzer®UAS-bla GripTite™ 293 cell line. GeneBLAzer®UAS-bla GripTite™ 293 cells stably express a betalactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-ER beta (LBD) fusion protein, the protein binds to the UAS, resulting in expression of beta-lactamase. Division Arrested (DA) cells are available in two configurations- an Assay Kit (which includes cells and sufficient substrate to analyze 1 x 384-well plate), and a tube of cells sufficient to analyze 10 x 384-well plates. DA cells are irreversibly division arrested using a low-dose treatment of Mitomycin-C, and have no apparent toxicity or change in cellular signal transduction. Both ER beta DA cells and ER beta-UAS-bla GripTite™ 293 cells are functionally validated for Z' and EC50 concentrations of 17-beta Estradiol. In addition, ER beta-UAS-bla GripTite™ 293 cells have been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time. Additional testing data using alternate stimuli are also available.