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-N0791
    Tectoridin
    99.85%
    Tectoridin is a isoflavone isolated from Maackia amurensis. Tectoridin is a phytoestrogen and activates estrogen and thyroid hormone receptors. Tectoridin exerts the estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway.
    Tectoridin
  • HY-N6678
    Zearalanone
    Activator 99.96%
    Zearalenone is a nonsteroidal estrogenic mycotoxin produced by Fusarium species, which colonizes several grains. Zearalenone has low acute toxicity and carcinogenicity. Due to its agonistic effect on the estrogen receptor, Zearalenone exhibits distinct estrogenic and anabolic properties in several animal species, resulting in severe effects on the reproductive system.
    Zearalanone
  • HY-I0508
    Phthalic acid
    Antagonist 99.92%
    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
  • HY-132247
    ErSO
    Activator 99.95%
    ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.
    ErSO
  • HY-13636R
    Fulvestrant (Standard)
    Antagonist 99.71%
    Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. 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.
    Fulvestrant (Standard)
  • HY-145341
    GNE-149
    Antagonist 99.66%
    GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
    GNE-149
  • HY-N0322R
    Cholesterol (Standard)
    Agonist 98.23%
    Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making 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.
    Cholesterol (Standard)
  • HY-101271
    WAY-200070
    Agonist 99.57%
    WAY-200070 is a selective estrogen receptor β (ERβ) agonist with an IC50 of 2.3 nM.
    WAY-200070
  • HY-B0723
    Ospemifene
    Modulator 99.84%
    Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
    Ospemifene
  • HY-W006405
    Isoflavone
    Isoflavone is an orally available bioactive component of soy phytoestrogen with lipid-lowering and antioxidant activities. Isoflavone prevents a variety of chronic diseases by regulating fatty acid oxidation in the liver and gene expression in adipose tissue. In addition, isoflavone has important value in the research of cancer and cardiovascular diseases.
    Isoflavone
  • HY-12870A
    AZD9496 maleate
    Antagonist 99.35%
    AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
    AZD9496 maleate
  • HY-148789
    Palazestrant
    Antagonist 98.96%
    Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER+/HER2+ cancer.
    Palazestrant
  • HY-108414
    (R)-Equol
    Agonist 98.93%
    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
    (R)-Equol
  • HY-113293BS1
    Estrone sulfate-d4 sodium
    99.38%
    Estrone sulfate-d4 (sodium) is deuterium labeled Estrone sulfate (sodium). Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
    Estrone sulfate-d<sub>4</sub> sodium
  • HY-118861A
    Enclomiphene citrate
    Antagonist 99.96%
    Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene citrate can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
    Enclomiphene citrate
  • HY-103454B
    MPP hydrochloride
    Modulator 99.28%
    MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
    MPP hydrochloride
  • HY-B0005A
    Toremifene
    Modulator 99.86%
    Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
    Toremifene
  • HY-B1234
    Octinoxate
    Modulator 99.89%
    Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate
  • HY-15731
    Estetrol
    Modulator 99.62%
    Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research.
    Estetrol
  • HY-101405
    Gestrinone
    Inhibitor 99.76%
    Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM. Gestrinone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Gestrinone
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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