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    • About
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Estrogen Receptor Beta (ERβ; NR3A2)

Product Family Product Number Product Description Technical Manual
IB0041
ERβ
(NR3A2)
IB00411-32 Human ERβ Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual
IB00411 Human ERβ Reporter Assay System, 1 x 96-well format assays Technical Manual
IB00412 Human ERβ Reporter Assay System, 1 x 384-well format assays
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This Estrogen Receptor Beta (ERβ) kit is an all-inclusive assay system that includes, in addition to ERβ 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.

ERβ 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.

INDIGO’s assay kits feature a luciferase detection reagent specially formulated to provide stable light emission between 5 and 90+ minutes after initiating the luciferase reaction. Incorporating a 5-minute reaction-rest period ensures that light emission profiles attain maximal stability, thereby allowing assay plates to be processed in batch. By doing so, the signal output from all sample wells, from one plate to the next, may be directly compared within an experimental set.

Kits are offered in different assay formats to accommodate researchers’ needs: 3 x 32, 1 x 96, and 1 x 384 assay formats for screening small numbers of test compounds, as well as custom bulk reagents for HTS applications.

Estrogen Receptor Beta Agonist AssayEstrogen Receptor Beta Antagonist Assay

Assay Kit & Platforms

Bulk assay reagents can be custom manufactured to accommodate any scale of HTS. Please inquire.

Estrogen receptor beta (ER-beta), also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2), is a nuclear receptor which is activated by the sex hormone estrogen. ER beta is encoded by the human gene ESR2 (Estrogen Receptor 2). This gene encodes a member of the family of estrogen receptors and superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17beta-estradiol or related ligands, the encoded protein forms homo- or hetero-dimers that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants has not been fully characterized. ERβ is expressed by many tissues including blood monocytes and tissue macrophages, colonic and pulmonary epithelial cells and in prostatic epithelium and in malignant counterparts of these tissues. ERβ may have anti-proliferative effects and therefore oppose the actions of ERα in reproductive tissue. ERβ may also have an important role in adaptive function of the lung during pregnancy.

INDIGO's Estrogen Receptor Beta Reporter Assay Systems utilize non-human mammalian cells engineered to express human ESR2, commonly referred to as NR3A2 or ERβ.

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 estrogen receptor beta.

For more information on ERβ, 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.

Steroid Receptor; Osteoporosis; Obesity; Cancer; Alzheimer’s Disease; Cardiovascular Disease; Reproduction and Development; Endocrinology; Environmental Toxicology

Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment

ABSTRACT While studying the environmental fate of potent endocrine-active steroid hormones, we observed the formation of an intramolecular [2+2] photocycloaddition product (2) with a novel hexacyclic ring system following photolysis of altrenogest (1). The structure and absolute configuration were established by X-ray diffraction analysis. Theoretical computations identified a barrierless two-step cyclization mechanism for the formationRead More

Posted in New Publications | Tagged androgen receptor, AR, endocrine-active steroid hormones, er, estrogen receptor, pregnane x receptor, PXR | Comments Off on Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment

Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity

ABSTRACT With many cancers showing resistance to current chemotherapies, the search for novel anti-cancer agents is attracting considerable attention. Natural flavonoids have been identified as useful leads in such programmes. However, since an in-depth understanding of the structural requirements for optimum activity is generally lacking, further research is required before the full potential of flavonoids as anti-proliferative agentsRead More

Posted in New Publications | Tagged er | Comments Off on Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity

Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity

ABSTRACT With many cancers showing resistance to current chemotherapies, the search for novel anti-cancer agents is attracting considerable attention. Natural flavonoids have been identified as useful leads in such programmes. However, since an in-depth understanding of the structural requirements for optimum activity is generally lacking, further research is required before the full potential of flavonoidsRead More

Posted in New Publications | Tagged er | Comments Off on Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity

Phytoestrogenic activity of blackcurrant (Ribes nigrum) anthocyanins is mediated through estrogen receptor alpha

ABSTRACT Blackcurrants (Ribes nigrum L., Grossulariaceae) contain high amounts of anthocyanin polyphenols, which have antioxidant and anti-carcinogenic health benefits. This study analyzed the potential phytoestrogenic effects of blackcurrant extract (BCE) in breast cancer (MCF-7) and human endometrial cancer (Ishikawa) cell lines that over-express estrogen receptor alpha (ERα), as well as in immature female rats. ToRead More

Posted in New Publications | Tagged er | Comments Off on Phytoestrogenic activity of blackcurrant (Ribes nigrum) anthocyanins is mediated through estrogen receptor alpha

Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor

ABSTRACT Breast cancer cells express enzymes that convert cholesterol, the synthetic precursor of steroid hormones, into estrogens and androgens, which then drive breast cancer cell proliferation. In the present study, we sought to determine whether oxidosqualene cyclase (OSC), an enzyme in the cholesterol biosynthetic pathway, may be targeted to suppress progression of breast cancer cells. In previous studies, weRead More

Posted in New Publications | Tagged AR, er | Comments Off on Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor

Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation

ABSTRACT The RAR-related orphan receptor gamma t (RORγt) is a nuclear receptor required for generating IL-17–producing CD4+ Th17 T cells, which are essential in host defense and may play key pathogenic roles in autoimmune diseases. Oxysterols elicit profound effects on immune and inflammatory responses as well as on cholesterol and lipid metabolism. Here, we describe the identification of several naturally occurringRead More

Posted in New Publications | Tagged CAR, er, FXR, GR, PPAR, PPARα, PPARβ, PPARγ, ROR, RORγ, RORγt | Comments Off on Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation

Probing the human estrogen receptor-a binding requirements for phenolic mono- and di-hydroxyl compounds: A combined synthesis, binding and docking study

ABSTRACT Various estrogen analogs were synthesized and tested for binding to human ERα using a florescence polarization displacement assay. Binding affinity and orientation were also predicted using docking calculations. Docking was able to accurately predict relative binding affinity and orientation for estradiol, but only if a tightly bound water molecule bridging Arg394/Glu353 is present. Di-hydroxylRead More

Posted in New Publications | Tagged er | Comments Off on Probing the human estrogen receptor-a binding requirements for phenolic mono- and di-hydroxyl compounds: A combined synthesis, binding and docking study

Structural Stereochemistry of Androstane Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoids Receptors

ABSTRACT DHEA, 17α-AED, 17β-AED, and 17β-AET exhibit strong biological activity that has been attributed to androgenic, estrogenic, or antiglucocorticoid activity in vivo and in vitro. This study compared DHEA, 17α-AED, 17β-AED, and 17β-AET for their ability to activate the human AR, ER, and GR and determine the relative androgenicity, estrogenicity, and glucocorticoid activity. The results show that, at theRead More

Posted in New Publications | Tagged AR, er, GR | Comments Off on Structural Stereochemistry of Androstane Hormones Determines Interactions with Human Androgen, Estrogen, and Glucocorticoids Receptors
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