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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 (141):

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. Tamoxifen activates autophagy and induces apoptosis.
  • HY-13636
    Fulvestrant Antagonist 99.99%
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
  • HY-B0141
    Estradiol Agonist 99.99%
    Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-16950
    4-Hydroxytamoxifen Modulator 99.89%
    4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
  • 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-133017
    SAR439859 Antagonist 99.25%
    SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer.
  • 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-109176
    Giredestrant Antagonist
    Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
  • HY-13757
    Tamoxifen Citrate Modulator 99.55%
    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. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • 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-12870
    AZD9496 Antagonist 99.15%
    AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD).
  • HY-N0322
    Cholesterol Agonist >98.0%
    Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  • HY-103456
    PHTPP Antagonist 99.07%
    PHTPP is a selective ERβ antagonist.
  • 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-103449
    G15 Antagonist >99.0%
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  • HY-A0036
    Bazedoxifene acetate Modulator 99.93%
    Bazedoxifene acetate (TSE-424 acetate) is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
  • HY-13738A
    Raloxifene hydrochloride Antagonist 99.94%
    Raloxifene hydrochloride (LY156758 hydrochloride; LY139481 hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
  • HY-12452
    DPN Activator 99.66%
    DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β(ER β) selective ligand.
  • 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.
Isoform Specific Products

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