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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.

Estrogen Receptor/ERR Isoform Specific Products:

  • Estrogen receptor

  • ERα

  • ERβ

  • ERRα

  • ERRβ

  • ERRγ

Estrogen Receptor/ERR Related Products (119):

Cat. No. Product Name Effect Purity
  • HY-13757A
    Tamoxifen Modulator 99.95%
    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-13636
    Fulvestrant Inhibitor 99.99%
    Fulvestrant (ICI 182780; ZD 9238; ZM 182780) is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
  • HY-B0141
    Estradiol Agonist 99.99%
    Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
  • HY-16950
    4-Hydroxytamoxifen Modulator 99.86%
    4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
  • HY-13757
    Tamoxifen Citrate Modulator >99.0%
    Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-111226
    GSK5182 Inhibitor
    GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces Reactive Oxyen Species (ROS) generation in hepatocellular carcinoma (HCC).
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one >98.0%
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride Antagonist 99.61%
    N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
  • HY-19822A
    Elacestrant dihydrochloride Inhibitor 99.81%
    Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-12870
    AZD9496 Antagonist 99.15%
    AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM.
  • HY-14590
    Kaempferol Inhibitor 99.62%
    Kaempferol inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK.
  • HY-107216
    G-1 Agonist 99.20%
    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
  • HY-103456
    PHTPP Antagonist 99.07%
    PHTPP is a selective ERβ antagonist.
  • HY-13738A
    Raloxifene hydrochloride Antagonist 99.94%
    Raloxifene hydrochloride (LY156758 hydrochloride; LY139481 hydrochloride) is a second generation selective estrogen receptor antagonist.
  • HY-A0036
    Bazedoxifene acetate Modulator 99.93%
    Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
  • HY-N0322
    Cholesterol Agonist >98.0%
    Cholesterol is the major sterol in mammals, and its importance in fundamental cellular processes is becoming more appreciated.
  • HY-10426
    XCT790 Antagonist 99.66%
    XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
  • HY-N2371
    27-Hydroxycholesterol Modulator 99.38%
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-B1192
    Estradiol benzoate Agonist 99.69%
    Estradiol Benzoate, a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
  • HY-B0234
    Estrone Agonist 99.86%
    Estrone is an estrogenic hormone.
Isoform Specific Products

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