Retinoid X Receptor Alpha (RXRα; NR2B1)
| Product Family | Product Number | Product Description | Technical Manual |
| IB0080 RXRα (NR2B1) |
IB00801-32 | Human RXRα Reporter Assay System, 3 x 32 assays in 96-well format | Technical Manual |
| IB00801 | Human RXRα Reporter Assay System, 1 x 96-well format assays | Technical Manual | |
| IB00802 | Human RXRα Reporter Assay System, 1 x 384-well format assays | Technical Manual |
Kits are offered in different assay formats to accommodate researchers’ needs: 3x 32, 1x 96, and 1x 384 assay formats for screening small numbers of test compounds, as well as custom bulk reagents for HTS applications. Assay systems are all inclusive, providing reporter cells, optimized growth media, media for diluting test compounds, a positive-control agonist, luciferase detection reagent, a white assay plate, a detailed protocol, and a protocol quick guide. All kits are shipped on dry ice.
RXRα Reporter Cells are prepared using INDIGO’s proprietary CryoMite™ process. This cryo-preservation method yields high cell viability post-thaw, and provides the convenience of immediately dispensing healthy, division-competent reporter cells into assay plates. There is no need for intermediate spin-and-wash steps, viability determinations, or cell titer adjustments.
This kit product is an all-inclusive assay system that includes, in addition to RXRα Reporter Cells, two optimized media for use during cell culture and (optionally) in diluting the test samples, a reference agonist, Luciferase Detection Reagent, a cell culture-ready assay plate, and a detailed protocol.
Bulk assay reagents can be custom manufactured to accommodate any scale of HTS. Please inquire.
INDIGO’s RXR Alpha Reporter Assay System utilizes non-human mammalian cells engineered to provide constitutive, high-level expression of Human Retinoid X Receptor Alpha (NR2B1), a ligand-dependent transcription factor commonly referred to as RXRA or RXRα. Additionally, these cells contain an RXRα-responsive luciferase reporter gene. Thus, quantifying luciferase activity provides a surrogate measure of RXRα activity in the treated reporter cells.
Retinoid X receptor alpha (RXRα), also known as NR2B1 is a nuclear receptor which in humans is encoded by the RXRA gene. Retinoid X receptors (RXRs) and retinoic acid receptors (RARs), are nuclear receptors that mediate the biological effects of retinoids by their involvement in retinoic acid-mediated gene activation. These receptors exert their action by binding, as homodimers or heterodimers, to specific sequences in the promoters of target genes and regulating their transcription. The protein encoded by this gene is a member of the steroid and thyroid hormone receptor superfamily of transcription factors.
For more information on RXRα, visit the Nuclear Receptor Resource.
Service Assays: Human
The primary application of INDIGO’s cell-based nuclear receptor assays are to quantitatively assess the bioactivity of a test compound as an agonist (activator) or antagonist (inhibition of an agonist response) of a given receptor. Service assays include a positive control reference compound and ‘vehicle’ control for every experiment. A formal study report and all data files are provided to the client upon completion of the study. To receive a quote for your proposed study, complete & submit the online “Request a Quote” form or contact an INDIGO Customer Service Representative to discuss your desired study parameters.
Disruption of Nuclear Receptor Signaling Alters Triphenyl Phosphate-Induced Cardiotoxicity in Zebrafish Embryos
ABSTRACT Triphenyl phosphate (TPHP) is an unsubstituted aryl phosphate ester used as a flame retardant and plasticizer within the United States. Using zebrafish as a model, the objectives of this study were to rely on (1) mRNA-sequencing to uncover pathways disrupted following embryonic TPHP exposure and (2) high-content screening to identify nuclear receptor ligands thatRead More
Systems toxicology identifies mechanistic impacts of 2-amino-4,6-dinitrotoluene (2A-DNT) exposure in Northern Bobwhite
ABSTRACT Background: A systems toxicology investigation comparing and integrating transcriptomic and proteomic results was conducted to develop holistic effects characterizations for the wildlife bird model, Northern bobwhite (Colinus virginianus) dosed with the explosives degradation product 2-amino-4,6-dinitrotoluene (2A-DNT). A subchronic 60d toxicology bioassay was leveraged where both sexes were dosed via daily gavage with 0, 3, 14, or 30 mg/kg-dRead More
β-apo-13-Carotenone Regulates Retinoid X Receptor Transcriptional Activity Through Tetramerization of the Receptor
ABSTRACT Retinoid X receptor (RXRα) is activated by 9-cis-retinoic acid (9cRA) and regulates transcription as a homodimer or as a heterodimer with other nuclear receptors. We have previously demonstrated that β-apo-13-carotenone, an eccentric cleavage product of β-carotene, antagonizes the activation of RXRα by 9cRA in mammalian cells overexpressing this receptor. However, the molecular mechanism ofRead More
Examination of Retinoid-like Compounds for Human RXRs, RARs, and RORs
View Full Size Research conducted by: Prajakta Albrecht (1), Koji Toyokawa (1), Ewa Maddox (1), Palmer Cramer (1), Jack Vanden Huevel (1,2), & Bruce Sherf (1) (1) INDIGO Biosciences, Inc., 1981 Pine Hall Rd, State College, PA, USA (2) Center for Molecular Toxicology and Carcinogenesis, 325 Life Sciences Building, Penn State University, University Park, PA 16802,Read More
Examination of Specificity of Retinoid-like Compounds for Human RXRs, RARs, and RORs
ABSTRACT Vitamin A (retinol) and its metabolites play many physiological roles including cell differentiation, cell proliferation, energy homeostasis, circadian rhythm and immune response. Vitamin A and its metabolites are known to act through retinoid acid receptors (RARs), retinoid-related orphan receptors (RORs) and retinoid x receptors (RXRs). These receptors are also important drug targets, although theRead More
Regulation of inflammatory and lipid metabolism genes by eicosapentaenoic acid-rich oil
ABSTRACT Omega-3-PUFAs, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), are associated with prevention of various aspects of metabolic syndrome. In the present studies, the effects of oil rich in EPA on gene expression and activation of nuclear receptors was examined and compared with other 3-PUFAs. The EPA-rich oil (EO) altered the expression of FA metabolism genes in THP-1 cells, including stearoylRead More
Differential Activation of Nuclear Receptors by Perflunoriated Fatty Acid Analogs and Natural Fatty Acids: A Comparison of Human, Mouse, and Rat Peroxisome Proliferator-Activated Receptor Receptor-a, -b, and -c, Liver X Receptor-b, and Retinoid X Receptor-a
ABSTRACT Administration of ammonium salts of perfluorooctanoate (PFOA) to rats results in peroxisome proliferation and benign liver tumors, events associated with activation of the nuclear receptor (NR) peroxisome proliferator-activated receptor-a (PPARa). Due to its fatty acid structure, PFOA may activate other NRs, such as PPARb, PPARg, liver X receptor (LXR), or retinoid X receptor (RXR). In this study, theRead More