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-N15473
    Isopaucifloral F
    Agonist
    Isopaucifloral F ((±)-Isopaucifloral F) is a Resveratrol (HY-16561)-derived sesquiterpenes. Isopaucifloral F is an orally active ERβ agonist (EC50: 46.96 μM). Isopaucifloral F has antiosteoporosis activity. LD50 in rats: > 5 mg/kg.
    Isopaucifloral F
  • HY-118861AS1
    Clomiphene-d5 citrate
    Antagonist
    Clomiphene-d5 (citrate) is the deuterium labeled Enclomiphene citrate. Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
    Clomiphene-d<sub>5</sub> citrate
  • HY-113293BR
    Estrone sulfate sodium (Standard)
    Estrone sulfate (sodium) (Standard) is the analytical standard of Estrone sulfate (sodium). This product is intended for research and analytical applications. 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). Estrone sulfate can be used for the research of breast cancer.
    Estrone sulfate sodium (Standard)
  • HY-B0141S6
    Estradiol-d2-1
    Agonist
    Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
    Estradiol-d<sub>2</sub>-1
  • HY-B0005R
    Toremifene citrate (Standard)
    Modulator
    Toremifene (citrate) (Standard) is the analytical standard of Toremifene (citrate). This product is intended for research and analytical applications. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
    Toremifene citrate (Standard)
  • HY-108293R
    Promestriene (Standard)
    Agonist
    Promestriene (Standard) is the analytical standard of Promestriene. This product is intended for research and analytical applications. Promestriene is a synthetic diethyl-ether of estradiol and a locally effective estrogen. Promestriene has an efficient action on vaginal atrophy while it is minimally absorbed.
    Promestriene (Standard)
  • HY-163712
    17-Epiestriol
    Agonist
    17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase.
    17-Epiestriol
  • 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-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
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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