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-16950R
    4-Hydroxytamoxifen (Standard)
    Modulator
    4-Hydroxytamoxifen (Standard) is the analytical standard of 4-Hydroxytamoxifen. This product is intended for research and analytical applications. 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is also the active metabolic form of Tamoxifen (HY-13757A) in vivo and can be used to induce gene knockout in transgenic mice expressing CreER.
    4-Hydroxytamoxifen (Standard)
  • 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-W013935R
    Bisphenol B (Standard)
    Agonist
    Bisphenol B (Standard) is the analytical standard of Bisphenol B. This product is intended for research and analytical applications. Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties.
    Bisphenol B (Standard)
  • 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 99.79%
    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-116896R
    LY117018 (Standard)
    Modulator
    LY117018 (Standard) is the analytical standard of LY117018. This product is intended for research and analytical applications. LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
    LY117018 (Standard)
  • 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-A0037R
    Lasofoxifene (Standard)
    Lasofoxifene (Standard) is the analytical standard of Lasofoxifene. This product is intended for research and analytical applications. Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis.
    Lasofoxifene (Standard)
  • 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.
    PHTPP (Standard)
  • HY-N6709R
    Zeranol (Standard)
    Agonist
    Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
    Zeranol (Standard)
  • HY-N11785
    Glyceollin I
    Modulator
    Glyceollin I is a selective estrogen receptor (ER) modulator with anticancer, antioxidant, and anti-inflammatory activities. Glyceollin I is promising for research of estrogen-related cancers (e.g., breast, ovarian) and metabolic disorders (e.g., hypercholesterolemia).
    Glyceollin I
  • HY-P991358
    XOMA-213
    Inhibitor
    XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting PRLR/Prolactin Receptor. XOMA-213 inhibits hPRL-dependent growth of BaF3/hPRLR cells (EC50: 0.5 μg/mL). XOMA-213 inhibits PRLR signaling and tumor growth in the Nb2-11-luc xenograft mouse model and the DMBA-induced rat breast cancer model. XOMA-213 can be used in Breast cancer, Hyperprolactinaemia and Prostate cancer research.
    XOMA-213
  • 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-12452R
    DPN (Standard)
    Agonist
    DPN (Standard) is the analytical standard of DPN. This product is intended for research and analytical applications. DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.
    DPN (Standard)
  • HY-B1100R
    Estradiol cypionate (Standard)
    Inhibitor
    Estradiol cypionate (Standard) is the analytical standard of Estradiol cypionate. This product is intended for research and analytical applications. Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.
    Estradiol cypionate (Standard)
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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