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-B1361R
    Estropipate (Standard)
    Agonist
    Estropipate (Standard) is the analytical standard of Estropipate. This product is intended for research and analytical applications.
    Estropipate (Standard)
  • HY-103451A
    rel-(R,R)-THC
    Antagonist
    rel-(R,R)-THC is the relative configuration of (R,R)-THC (HY-103451). (R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6.
    rel-(R,R)-THC
  • HY-137818
    SR19881
    Agonist
    SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively.
    SR19881
  • HY-149970
    ER degrader 5
    Degrader
    ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer.
    ER degrader 5
  • HY-19822S
    Elacestrant-d4
    Inhibitor
    Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER+ breast cancer cell lines both in vitro and in vivo.
    Elacestrant-d<sub>4</sub>
  • HY-N0250R
    Saikosaponin D (Standard)
    Activator
    Saikosaponin D (Standard) is the analytical standard of Saikosaponin D. This product is intended for research and analytical applications. Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
    Saikosaponin D (Standard)
  • HY-B1403S
    Dienestrol-d2
    Agonist
    Dienestrol-d2 is a deuterium labeled Dienestrol (HY-B1403).
    Dienestrol-d<sub>2</sub>
  • HY-124403
    D 15413
    Inhibitor
    D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10-7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer.
    D 15413
  • HY-135582S1
    Raloxifene 4'-glucuronide-d4 lithium
    Modulator
    Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. 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. [1][2]. 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[3].
    Raloxifene 4'-glucuronide-d<sub>4</sub> lithium
  • HY-N6052
    (+)-Medicarpin
    Activator
    (+)-Medicarpin, a pterocarpan, is a type of isoflavonoid isolated from several medicinal plant species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum, Platymiscium floribundum, and so on. (+)-Medicarpin potently inhibits osteoclastogenesis and promotes bone healing and increases bone mass by osteoblast differentiation with estrogen receptor (ER) β-mediated osteogenic action.
    (+)-Medicarpin
  • HY-163766
    Antiproliferative agent-51
    Inhibitor
    Antiproliferative agent-51 (Compound 18h) exhibits inhibitory efficacy against estrogen receptor α (ERα) mediated transcription, with an IC50 of 1.6 nM. Antiproliferative agent-51 inhibits the proliferation of cancer cell ZR-75, with an IC50 of 0.031 μM. Antiproliferative agent-51 exhibits antitumor efficacy in mouse models.
    Antiproliferative agent-51
  • HY-B1662S2
    (Rac)-Hexestrol-d6 (hexane-2,2,3,4,5,5-d6)
    (Rac)-Hexestrol-d6 (hexane-2,2,3,4,5,5-d6) is the deuterium labeled (Rac)-Hexestrol (hexane-2,2,3,4,5,5)[1].
    (Rac)-Hexestrol-d<sub>6</sub> (hexane-2,2,3,4,5,5-d6)
  • HY-100327
    MK-6913
    Agonist
    MK-6913 (Tetrahydrofluoroene 52) is a potent and selective estrogen receptor β agonist.
    MK-6913
  • HY-144202
    Estrogen receptor antagonist 4
    Antagonist
    Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1).
    Estrogen receptor antagonist 4
  • HY-113251S1
    2-Hydroxyestrone-13C6
    Inhibitor
    2-Hydroxyestrone-13C6 is the 13C-labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
    2-Hydroxyestrone-<sup>13</sup>C<sub>6</sub>
  • HY-B0390S1
    Mestranol-d4
    Agonist
    Mestranol-d4 is the deuterium labeled Mestranol. Mestranol is an inactive proagent and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders[1][2][3]. Mestranol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mestranol-d<sub>4</sub>
  • HY-135590
    Raloxifene 4-Monomethyl Ether
    Modulator
    Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6.
    Raloxifene 4-Monomethyl Ether
  • HY-N6710R
    α-Zearalenol (Standard)
    Inhibitor
    α-Zearalenol (Standard) is the analytical standard of α-Zearalenol. This product is intended for research and analytical applications. α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.
    α-Zearalenol (Standard)
  • HY-B0412S4
    Estriol-d3-1
    Antagonist
    Estriol-d3-1 is the deuterium labeled Estriol.
    Estriol-d<sub>3</sub>-1
  • HY-123047R
    Tibolone (Standard)
    Agonist
    Tibolone (Standard) is the analytical standard of Tibolone. This product is intended for research and analytical applications. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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