1. Signaling Pathways
  2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR

Estrogen Receptor/ERR

Estrogen receptors are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and GPER (GPR30), which is a member of the rhodopsin-like family of G protein-coupled receptors. The ER's helix 12 domain plays a crucial role in determining interactions with coactivators and corepressors and, therefore, the respective agonist or antagonist effect of the ligand. Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors, estrone, and raloxifene bind preferentially to the alpha receptor, estriol, and genistein to the beta receptor. Estrogen and its receptors are essential for sexual development and reproductive function, but also play a role in other tissues such as bone. Estrogen receptors are also involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. Alternative promoter usage and alternative splicing result in dozens of transcript variants, but the full-length nature of many of these variants has not been determined.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-135582
    Raloxifene 4'-glucuronide
    Modulator
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
    Raloxifene 4'-glucuronide
  • HY-N6714R
    Alternariol (Standard)
    Activator
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol (Standard)
  • HY-B1012R
    Quinestrol (Standard)
    Agonist
    Quinestrol (Standard) is the analytical standard of Quinestrol. This product is intended for research and analytical applications. Quinestrol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Quinestrol (Standard)
  • HY-153001
    MK-8389
    Agonist
    MK-8389 is an orally active LMW allosteric FSH receptor agonist. MK-8389 affects thyroid function.
    MK-8389
  • HY-W752886
    Estradiol 3-d3 (β-D-Glucuronide) sodium
    Estradiol 3-d3 (β-D-Glucuronide) sodium is the deuterium labeled Estradiol 3-(β-D-Glucuronide) sodium (HY-N7755). Estradiol 3-(β-D-Glucuronide) sodium is the glucuronic acid derivative of estradiol (HY-B0141). Estradiol 3-(β-D-Glucuronide) sodium is radiolabeled for use in tumor imaging and biodistribution studies.
    Estradiol 3-d<sub>3</sub> (β-D-Glucuronide) sodium
  • HY-107803
    Geranium oil
    Agonist
    Geranium oil serves as a partial agonist for estrogen receptor (ER), enhancing both the cytotoxicity induced by Tamoxifen (TMX) (HY-13757A) in GT1-7 cells and the adverse effects of TMX on the central nervous system. Geranium oil can be utilized in the research of neurological disorders such as dementia.
    Geranium oil
  • HY-146440
    LSD1/ER-IN-1
    Inhibitor
    LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM.
    LSD1/ER-IN-1
  • HY-126932
    TTC-352
    Agonist
    TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites.
    TTC-352
  • HY-153700
    Estrogen receptor modulator 8
    Inhibitor
    Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM.
    Estrogen receptor modulator 8
  • HY-W009301R
    6-Ketoestradiol (Standard)
    6-Ketoestradiol (Standard) is the analytical standard of 6-Ketoestradiol. This product is intended for research and analytical applications. 6-Ketoestradiol can be used to synthesize re-containing 7α-substituted estradiol complexes.
    6-Ketoestradiol (Standard)
  • HY-W106688
    Triisopropyl phosphate
    Antagonist
    Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression, exhibits anti-estrogenic activity that inhibits Estradiol (HY-B0141)-induced MCF-7 cell proliferation with an EC50 of 341 μM. Triisopropyl phosphate inhibits the estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM.
    Triisopropyl phosphate
  • HY-N2371R
    27-Hydroxycholesterol (Standard)
    Modulator
    27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.
    27-Hydroxycholesterol (Standard)
  • HY-I0508R
    Phthalic acid (Standard)
    Antagonist
    Phthalic acid (Standard) is the analytical standard of Phthalic acid. This product is intended for research and analytical applications. Phthalic acid is the final common metabolite of phthalic acid esters (PAEs). Phthalic acid can be used for the synthesis of synthetic agents, such as isophthalic acid (IPA), and terephthalic acid (TPA). Phthalic acid has applications in the preparation of phthalate ester plasticizers. Phthalic acid exhibits mutagenic effect and causes genetic damage in mammalian germ cells.
    Phthalic acid (Standard)
  • HY-123047S
    Tibolone-d5
    Agonist
    Tibolone-d5 is deuterium labeled Tibolone. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone-d<sub>5</sub>
  • HY-W114419
    Bisphenol C
    Modulator ≥98.0%
    Bisphenol C is an estrogen receptor-α (ERα) agonist and an ERβ antagonist, with IC50 values of 2.65 nM for ERα and 1.94 nM for ERβ. Bisphenol C is a material of manufacturing polyester polymers like polycarbonate, is widely used in daily items like water bottles, food packaging, textile and so on.
    Bisphenol C
  • HY-19822S1
    Elacestrant-d4-1
    Inhibitor
    Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
    Elacestrant-d<sub>4</sub>-1
  • HY-B2158R
    Chlorotrianisene (Standard)
    Modulator
    Chlorotrianisene (Standard) is the analytical standard of Chlorotrianisene. This product is intended for research and analytical applications. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
    Chlorotrianisene (Standard)
  • HY-B0005S
    Toremifene-d6 citrate
    Modulator
    Toremifene-d6 (citrate) is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively.
    Toremifene-d<sub>6</sub> citrate
  • HY-W326021
    Phenolphthalol
    Activator
    Phenolphthalol is a laxative in agent preparations and also estrogenically active.
    Phenolphthalol
  • HY-116939
    (E)-Broparestrol
    Activator
    (E)-Broparestrol is a biologically active tetrasubstituted olefin, which is used as an estrogen in dermatology.
    (E)-Broparestrol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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