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-171477
    Metahexestrol
    Ligand
    Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer.
    Metahexestrol
  • HY-125091
    LY2066948
    LY2066948 is a selective and orally active estrogen receptor modulator (SERM). LY2066948 has high affinity for estrogen receptors ERα and ERβ (Ki: 0.51 and 1.36 nM respectively) and shows potent antiestrogenic activity. LY2066948 blocks uterine weight gain induced by Ethynyl estradiol (HY-B0216) in immature rats. LY2066948 can be used for research of uterine fibroids and myomas.
    LY2066948
  • HY-103447S2
    Zearalenone-13C7
    Activator
    Zearalenone-13C7 (Mycotoxin F2-13C7) is 13C labeled Zearalenone. Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts.
    Zearalenone-<sup>13</sup>C<sub>7</sub>
  • HY-B0141C
    Estradiol hemihydrate
    Agonist
    Estradiol (β-Estradiol) hemihydrate is a steroid hormone and the major female sex hormone. Estradiol (β-Estradiol) hemihydrate can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol (β-Estradiol) hemihydrate can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering.
    Estradiol hemihydrate
  • HY-121372
    Lactandrate
    Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1.
    Lactandrate
  • HY-B1234A
    (E)-Octinoxate
    Inhibitor
    (E)-Octinoxate is the isomer of Octinoxate (HY-B1234). Octinoxate is an organic compound that is an ingredient in some sunscreens and lip balms, primarily used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage and can be used to reduce the appearance of scars. Octinoxate also has a complex androgenic and estrogenic effect.
    (E)-Octinoxate
  • HY-103456R
    PHTPP (Standard)
    Antagonist
    PHTPP (Standard) is the analytical standard of PHTPP. This product is intended for research and analytical applications. PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα[1].
    PHTPP (Standard)
  • HY-13757R
    Tamoxifen (Citrate) (Standard)
    Modulator
    Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. Tamoxifen Citrate (ICI 46474) is an orally active, 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 also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen (Citrate) (Standard)
  • HY-W338581
    4-tert-Octylphenol monoethoxylate
    4-tert-Octylphenol monoethoxylate is an alkylphenolethoxylate (APE) and a degradation product of non-ionic surfactants (such as 4-tert-octylphenol polyethoxylate). 4-tert-Octylphenol monoethoxylate also possesses non-steroidal estrogenic activity. Additionally, 4-tert-Octylphenol monoethoxylate has been found in wastewater effluent.
    4-tert-Octylphenol monoethoxylate
  • HY-169941
    ERα/ERβ antagonist-1
    Antagonist
    ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and ERβ. ERα/ERβ antagonist-1 reduces ERα and ERβ activity in a dose-dependent manner in HepG2 liver cells.
    ERα/ERβ antagonist-1
  • HY-N1875
    4-(Ethoxymethyl)phenol
    Agonist 98.02%
    4-(Ethoxymethyl)phenol (p-Hydroxybenzyl Et ether) is a potent antioxidant from Amburana cearensis leaf extract, with in vitro cytogenotoxic properties. Amburana cearensis leaves can be used foe the research of respiratory diseases and inflammations.
    4-(Ethoxymethyl)phenol
  • HY-N13076
    Neo-sagittasine A
    Neo-sagittasine A (compound 2) is an estrogen biosynthesis promoter that can enhance estrogen biosynthesis in human ovarian granulosa-like KGN cells. Neo-sagittasine A can be isolated from Epimedium brevifolium.
    Neo-sagittasine A
  • HY-W011100R
    Cyclofenil (Standard)
    Modulator
    Cyclofenil (Standard) is the analytical standard of Cyclofenil. This product is intended for research and analytical applications. Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
    Cyclofenil (Standard)
  • HY-W009066
    2-Ethylhexyl diphenyl phosphate
    Inhibitor
    2-Ethylhexyl diphenyl phosphate is an organophosphate flame retardants (OPFRs) and a PPARG agonist (EC20: 2.04 µM). 2-Ethylhexyl diphenyl phosphate also inhibits ERRγ transcriptional activity (IC50: 1.3 µM). 2-Ethylhexyl diphenyl phosphate upregulates 3β-HSD1, human chorionic gonadotropin (hCG) and progesterone secretion. 2-Ethylhexyl diphenyl phosphate can be used in studies of female reproduction and fetal development.
    2-Ethylhexyl diphenyl phosphate
  • HY-138089
    17β-Hydroxy exemestane
    Agonist
    17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
    17β-Hydroxy exemestane
  • HY-N13290
    10-Chloroestra-1,4-diene-3,17-dione
    Control
    10-Chloroestra-1,4-diene-3,17-dione (10-CIEsra) is a derivative of estrogen receptor.
    10-Chloroestra-1,4-diene-3,17-dione
  • HY-B0845R
    Prochloraz (Standard)
    Antagonist
    Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz (Standard)
  • HY-121441
    Fispemifene
    Modulator
    Fispemifene, an orally active selective estrogen receptor modulator with anti-inflammatory and antiestrogenic action, attenuates glandular inflammation in an animal model of chronic nonbacterial prostatitis.
    Fispemifene
  • HY-100583R
    (-)-(S)-Equol (Standard)
    (-)-(S)-Equol (Standard) is the analytical standard of (-)-(S)-Equol. This product is intended for research and analytical applications. (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
    (-)-(S)-Equol (Standard)
  • HY-151230
    (-)-Erteberel
    Agonist
    (-)-Erteberel is a selective estrogen receptor beta (ERβ) agonist. (-)-Erteberel can be utilized in the study of diseases mediated by estrogen receptor beta (ERβ), such as prostate cancer.
    (-)-Erteberel
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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