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-N15342
    Tschimganidin
    Agonist
    Tschimganidin is an ERα agonist with an IC50 of 1.4 μM. Found in plants of the Apiaceae family, Tschimganidin is a terpenoid compound with anti-obesity activity. It can be used for research in the field of endocrine and metabolic disorders.
    Tschimganidin
  • HY-162838
    TCF199
    TCF199 is an allosteric stabilizer that stabilizes the 14-3-3/TAZ peptide interaction, binding to the 14-3-3ζ/E R α peptide and 14-3-3ζ/Chibby peptide. TCF199 has a Kd value of 122 μM for its interaction with 14-3-3/TAZ.
    TCF199
  • HY-49537
    ER ligand-10
    Ligand
    ER ligand-10 (Compound 11a) is a weak ERa and ERβ ligand, and shows weak estrogenic activity.
    ER ligand-10
  • HY-101405R
    Gestrinone (Standard)
    Inhibitor
    Gestrinone (Standard) is the analytical standard of Gestrinone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B1234S
    Octinoxate-13C,d3
    Modulator
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). 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-<sup>13</sup>C,d<sub>3</sub>
  • 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-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-103454BR
    MPP hydrochloride (Standard)
    Modulator
    MPP hydrochloride (Standard) is the analytical standard of MPP hydrochloride (HY-103454B). This product is intended for research and analytical applications. 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 (Standard)
  • HY-W587442
    3-Chlorobisphenol A
    3-Chlorobisphenol A, a chlorinated derivatives of bisphenol A, is an endocrine-disrupting compound. It binds to estrogen receptors, causing disorders in hormone signaling pathways. Bisphenol A is an industrial chemical used in the production of polycarbonate plastics and epoxy resin.
    3-Chlorobisphenol A
  • 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 98.79%
    (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-183438
    Amsonic acid
    Ligand
    Amsonic acid is an orally active weak estrogen receptor ligand with uterotrophic activity. In the weanling female rat model, Amsonic acid exhibits a uterotrophic effect consistent with that of diethylstilbestrol at equiactive doses. Amsonic acid can also be used in studies related to erectile dysfunction.
    Amsonic acid
  • 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-107216R
    G-1 (Standard)
    Agonist
    G-1 (Standard) is the analytical standard of G-1 (HY-107216). This product is intended for research and analytical applications. G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
    G-1 (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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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