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Human GR Reporter Assay Kit

1 x 96-well format assays IB00201
3 x 32 assays in 96-well format IB00201-32
1 x 384-well format assays IB00202

Product Description and Product Data

This is an all-inclusive cell-based luciferase reporter assay kit targeting the Human Glucocorticoid Receptor (GR). INDIGO’s GR reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the Human GR. In addition to GR Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. The principal application of this assay is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against human GR. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture.


  • Clear, Reproducible Results

  • All-Inclusive Assay Systems
  • Exceptional Cell Viability Post-Thaw
  • Consistent Results Lot to Lot

Product Specifications

Target TypeNuclear Hormone Receptor
Receptor FormNative
Assay ModeAgonist, Antagonist
Kit Components
  • GR Reporter Cells
  • Cell Recovery Medium (CRM)
  • Compound Screening Medium (CSM)
  • Dexamethasone, (ref. agonist; in DMSO)
  • Detection Substrate
  • Detection Buffer
  • White, sterile, cell-culture ready assay plate
Shelf Life6 months
Orthologs AvailableYes
Shipping RequirementsDry Ice
Storage temperature-80C


Dose-response analyses of GR were performed according to the protocol provided in this Technical Manual. Reporter Cells were treated with: A.) the reference agonists Dexamethasone, Mometasone furoate, Fluticasone propionate, Budesonide, Methylprednisolone, GSK 9027, and Hydrocortisone or B.) a fixed EC80 concentration of the agonist dexamethasone and variable concentrations of the reference antagonists Mifepristone and AL082D06. (Dexamethasone is provided, all other chemicals from Cayman Chemical.) Luminescence was quantified and RLU values averaged. Respective values of % Activation and % Inhibition were calculated. GraphPad Prism software was used to perform the least squares method of non-linear regression and to determine EC50 values. RESULTS: The EC50 for dexamethasone is approximately 260 pM. Z’ values exceeded 0.74 for all reference compounds, thus confirming the robust performance of this Human GR assay and its suitability for use in HTS applications.

Target Background

The glucocorticoid receptor is the receptor that cortisol and other glucocorticoids bind to. The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response.

INDIGO’s Glucocorticoid Receptor Assay System utilize proprietary mammalian reporter cells engineered to provide constitutive high-level expression of full-length, unmodified human NR3C1 protein, commonly referred to as GR.

INDIGO’s Reporter Cells include the luciferase reporter gene functionally linked to a GR-responsive promoter. Thus, quantifying changes in luciferase expression in the treated reporter cells provides a sensitive surrogate measure of the changes in GR activity. Luciferase gene expression occurs after ligand-bound GR undergoes nuclear translocation, DNA binding, recruitment, and assembly of the co-activators and accessory factors required to forma functional transcription complex, culminating in expression of the reporter gene. Unlike some other cell-based assay strategies, the readout from INDIGO’s reporter cells demands the same orchestration of all intracellular molecular interactions and events that can be expected to occur in vivo.

The principle application of this assay product is in the screening of test samples to quantify functional activities, either agonist or antagonist, that they may exert against the human androgen receptor.


Tris(1,3-dichloro-2-propyl) phosphate (TDCPP) is an organophosphate flame retardant. The primary TDCPP metabolite, bis(1,3-dichloro-2-propyl) phosphate (BDCPP), is detectable in the urine of over 90 % of Americans. Epidemiological studies show sex-specific associations between urinary BDCPP levels and metabolic syndrome, which is an established risk factor for type 2 diabetes, heart disease, and stroke. We used a mouse model to determine whether TDCPP exposure disrupts glucose homeostasis. Six-week old male and female C57BL/6J mice were given ad libitum access to diets containing vehicle (0.1 % DMSO) and TDCPP resulting in the following treatment groups: 0 mg/kg/day, 0.02 mg/kg/day, 1 mg/kg/day, or 100 mg/kg/day. After being on the experimental diet for five weeks without interruption, body composition was analyzed, glucose and insulin tolerance tests were performed, and fasting glucose and insulin levels were quantified. TDCPP at 100 mg/kg/day caused male sex-specific adiposity, fasting hyperglycemia, and insulin resistance. TDCPP-induced modulation of nuclear receptor activation was investigated using an in vitro screen to identify potential mechanisms of metabolic disruption. TDCPP activated farnesoid X receptor (FXR) and pregnane X receptor (PXR), and inhibited the androgen receptor (AR). PXR target genes, but not FXR target genes, were upregulated in livers from mice exposed to 100 mg TDCPP/kg/day. Interestingly, PXR target genes were differentially expressed in livers from both males and females. It remains to be determined whether TDCPP-induced metabolic disruption occurs via modulation of nuclear receptor activity. Taken together, these studies build upon the association of TDCPP exposure and metabolic syndrome in humans by identifying sex-specific effects of TDCPP on glucose homeostasis in mice.
Cortisone is a metabolite belonging to the corticosteroid class that is used pharmaceutically directly as a drug or prodrug. In addition to its large consumption, its use is linked to several side effects, so pharmaceutical research aims to develop effective drugs with low or no side effects, alternative compounds to cortisone are part of an active investment in ongoing research on drug discovery. Since biotransformation can be considered a source of new molecules with potential therapeutic use, the present work focuses on a preliminary in vitro study aimed at evaluating the mutagenic, anti-inflammatory, antioxidant and neuroprotective activity of SCA and SCB molecules obtained from the biotransformation of cortisone using Rh. Rhodnii strain DSM 43960. The results obtained are very encouraging due to the safety of biotransformed compounds with reference to genotoxicity checked by Ames test, to the very high antioxidant capacity and to the anti-inflammatory activity. In fact, thecompounds inhibited both the TNFα-stimulated expression and secretion of NFkB target cytokines, and COX activity, and can activate the glucocorticoid receptor. Finally SCA and SCB exhibited neuroprotective properties.

Also available as a service

Glucocorticoid Receptor (GR, NR3C1)