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-16023
    Acolbifene hydrochloride
    Antagonist 99.00%
    Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
    Acolbifene hydrochloride
  • HY-P3833A
    Yp537 TFA
    Inhibitor
    Yp537 TFA is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor.
    Yp537 TFA
  • HY-U00300
    Cancer-Targeting Compound 1
    98.37%
    Cancer-Targeting Compound 1 is used in the research of hormone-?related cancer, extracted from patent WO 2008021331 A2.
    Cancer-Targeting Compound 1
  • HY-144070A
    (Rac)-ErSO-DFP
    Activator
    (Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1).
    (Rac)-ErSO-DFP
  • HY-135584
    Raloxifene 6-Monomethyl Ether
    Modulator
    Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6.
    Raloxifene 6-Monomethyl Ether
  • HY-13636A
    Fulvestrant (S enantiomer)
    Inhibitor
    Fulvestrant (ICI 182780; ZD 9238) S enantiomer is the S-enantiomer of Fulvestrant (HY-13636), a potent estrogen receptor inhibitor. Fulvestrant binds to and blocks the estrogen receptor, promotes its degradation, and thereby inhibits receptor dimerization, nucleocytoplasmic shuttling and transcriptional activity. Fulvestrant effectively blocks estrogen signaling, MAPK pathway activation and ER-regulated protein expression. Fulvestrant induces apoptosis, inhibits the proliferation of breast cancer and prolactinoma cells, and reduces the mineralization level, alkaline phosphatase activity and osteocalcin expression of preosteoblasts. Prenatal exposure to Fulvestrant impairs ovarian follicular development and causes ovarian structural damage. Fulvestrant has been widely used in studies related to breast cancer, prolactinoma and other conditions.
    Fulvestrant (S enantiomer)
  • HY-19468
    ERB-196
    Agonist 99.89%
    ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
    ERB-196
  • HY-N9329
    Glicoricone
    Antagonist
    Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity.
    Glicoricone
  • HY-135582
    Raloxifene 4'-glucuronide
    Modulator 98.19%
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
    Raloxifene 4'-glucuronide
  • HY-N2026R
    Propylparaben (Standard)
    Agonist
    Propylparaben (Propyl parahydroxybenzoate) (Standard) is the analytical standard of Propylparaben (HY-N2026). Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is an orally active weak estrogen receptor agonist. Propylparaben regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
    Propylparaben (Standard)
  • HY-W114419
    Bisphenol C
    Modulator ≥98.0%
    Bisphenol C is an estrogen receptor-α (ERα) agonist and an ERβ antagonist, with IC50 values of 2.65 nM for ERα and 1.94 nM for ERβ. Bisphenol C is a material of manufacturing polyester polymers like polycarbonate, is widely used in daily items like water bottles, food packaging, textile and so on.
    Bisphenol C
  • HY-N2026A
    Propylparaben sodium
    Agonist 99.03%
    Propylparaben (Propyl parahydroxybenzoate) sodium is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben sodium is an orally active weak estrogen receptor agonist. Propylparaben sodium regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben sodium is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
    Propylparaben sodium
  • HY-P991358
    XOMA-213
    Inhibitor 98.46%
    XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer.
    XOMA-213
  • HY-138089
    17β-Hydroxy exemestane
    Agonist 98.21%
    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-121441
    Fispemifene
    Modulator 99.67%
    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-W009160
    Octrizole
    99.67%
    Octrizole (UV-329) is a UV screener/stabilizer. Octrizole can prevent products from yellowing and degradation. Octrizole exhibits significant cytotoxicity to MVLN cells at concentrations higher than 50 μM and has no obvious estrogenic activity.
    Octrizole
  • HY-124414A
    4'-Hydroxytamoxifen TFA
    99.43%
    4'-Hydroxytamoxifen TFA is a salt form of a metabolite of Tamoxifen. 4'-Hydroxytamoxifen TFA has a higher affinity for ER than Tamoxifen. 4'-Hydroxytamoxifen TFA induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells.
    4'-Hydroxytamoxifen TFA
  • HY-B1234R
    Octinoxate (Standard)
    Modulator
    Octinoxate (Standard) is the analytical standard of Octinoxate. This product is intended for research and analytical applications. Octinoxate (Octyl methoxycinnamate) 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.
    Octinoxate (Standard)
  • HY-A0087R
    Octocrylene (Standard)
    Activator
    Octocrylene (Standard) is the analytical standard of Octocrylene. This product is intended for research and analytical applications. Octocrylene is an organic ultraviolet (UV) filter which absorbs mainly UVB radiation and short UVA wavelengths. Octocrylene has the potential for using in various cosmetic products to either provide an appropriate sun protection factor in sunscreen products or to protect cosmetic formulations from UV radiation.
    Octocrylene (Standard)
  • HY-15731S
    Estetrol-d4
    Modulator
    Estetrol-d4 is the deuterium labeled Estetrol. Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast.
    Estetrol-d<sub>4</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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