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-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-B1617AS2
    Zuclomiphene d10 Citrate salt
    Modulator
    Zuclomiphene d10 Citrate salt is deuterium labeled Zuclomiphene citrate (HY-B1617A). Zuclomiphene citrate is a cis isomer of Clomiphene citrate (HY-B0463). Zuclomiphene citrate is orally active and has an antiestrogenic effect. Zuclomiphene can reduce cholesterol levels. Zuclomiphene citrate can be for the researches of endocrinology and metabolic disease.
    Zuclomiphene d<sub>10</sub> Citrate salt
  • 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. . 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-d<sub>4</sub> lithium
  • HY-W753635
    EC 313
    Inhibitor
    EC 313 is a novel selective progesterone receptor modulator. EC 313 can dose dependently reduce the weight of fibroids. EC 313 can reduce the expression of ER and PR. EC 313 can be used for the study of uterine fibroids.
    EC 313
  • 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).
    (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-176486
    ER degrader 11
    Degrader
    ER degrader 11 (Compound 5) is an orally active, brain-penetrant and selective estrogen receptor (ER) degrader (ERα IC50=1.6 nM). ER degrader 11 is promising for research of breast cancer brain metastasis.
    ER degrader 11
  • 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.
    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. 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)
  • HY-106839
    NKS-01
    Modulator
    NKS-01 is a selective estrogen receptor modulator. NKS-01 can be used for the research of cancer, such as estrogen receptor-positive breast cancer.
    NKS-01
  • HY-149833
    ERRγ inverse agonist 2
    Agonist
    ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities.
    ERRγ inverse agonist 2
  • HY-169367
    ERD-1233
    Degrader
    ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER+ breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)).
    ERD-1233
  • HY-168099
    ERα degrader 10
    Degrader
    ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer.
    ERα degrader 10
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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