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-10830A
    PBPE hydrochloride
    99.30%
    PBPE hydrochloride is a derivative of tamoxifen (HY-13757A) and a selective ligand for the anti-estrogen binding site (AEBS), the binding affinities (Ki) of PBPE hydrochloride and MBPE to AEBS are 8.79 and 17.57 nM, respectively.
    PBPE hydrochloride
  • HY-144699
    ERRα antagonist-2
    Antagonist 99.07%
    ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.
    ERRα antagonist-2
  • HY-13738AR
    Raloxifene hydrochloride (Standard)
    Antagonist 99.84%
    Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
    Raloxifene hydrochloride (Standard)
  • 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-113251
    2-Hydroxyestrone
    Inhibitor 98.57%
    2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
    2-Hydroxyestrone
  • HY-137144
    Fulvestrant-3-boronic acid
    Inhibitor 99.7%
    Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells.
    Fulvestrant-3-boronic acid
  • HY-101119
    GLL398
    Degrader
    GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
    GLL398
  • HY-111226A
    (E/Z)-GSK5182
    Inhibitor 99.17%
    (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma.
    (E/Z)-GSK5182
  • HY-N0322S7
    Cholesterol-d1
    Agonist 99.29%
    Cholesterol-d1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
    Cholesterol-d<sub>1</sub>
  • HY-128838A
    (rel)-PROTAC ERRα Degrader-1
    98.18%
    (rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
    (rel)-PROTAC ERRα Degrader-1
  • HY-18719C
    Endoxifen E-isomer hydrochloride
    Inhibitor 98.20%
    Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects.
    Endoxifen E-isomer hydrochloride
  • HY-118860
    Corifollitropin alfa
    Agonist
    Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility.
    Corifollitropin alfa
  • HY-173178
    LNS8801
    Agonist
    LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes.
    LNS8801
  • HY-P5464
    SRC-1 NR box peptide
    SRC-1 NR box peptide is a biological active peptide (This peptide is a 14-amino acid fragment from the steroid receptor cofactor SRC-1 NR II). SRC-1 NR box peptide can be used to study the regulatory mechanisms of estrogen receptor ligands.
    SRC-1 NR box peptide
  • HY-13757S
    Tamoxifen-d3 hydrochloride
    Modulator 98.99%
    Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). 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-d<sub>3</sub> hydrochloride
  • HY-B1353
    Paroxypropione
    Inhibitor 99.97%
    Paroxypropione is a manufactured, nonsteroidal estrogen which has been used medically as an antigonadotropin.
    Paroxypropione
  • HY-B0487
    Ethisterone
    Agonist
    Ethisterone (Pregneninolone), a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone is reported for androgenic activity, used for the research of the gynecological disorders.
    Ethisterone
  • HY-144733
    ERα antagonist 1
    Antagonist
    ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells.
    ERα antagonist 1
  • HY-B1617AS
    Zuclomiphene-d4 citrate
    Modulator ≥99.0%
    Zuclomiphene-d4 (citrate) is a deuterium labeled Zuclomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.
    Zuclomiphene-d<sub>4</sub> citrate
  • HY-116896A
    LY117018 TFA
    Modulator 99.18%
    LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines.
    LY117018 TFA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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