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-118065
    Fenhexamid
    Agonist 99.60%
    Fenhexamid, a botryticide, is a sterol biosynthesis inhibitor. Fenhexamid shows fungicide efficient against the plant pathogenic fungus Botryotinia fuckeliana (Botrytis cinerea).
    Fenhexamid
  • HY-N0322S6
    Cholesterol-d4
    Agonist 99.26%
    Cholesterol-d4 is 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>4</sub>
  • HY-W011100
    Cyclofenil
    Modulator
    Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
    Cyclofenil
  • HY-14598S
    Diethylstilbestrol-d8
    Agonist 99.74%
    Diethylstilbestrol-d8 is the deuterium labeled Diethylstilbestrol. Diethylstilbestrol, a synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders.
    Diethylstilbestrol-d<sub>8</sub>
  • HY-B1012
    Quinestrol
    Agonist 99.72%
    Quinestrol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Quinestrol
  • HY-147402A
    Taragarestrant meglumine
    Degrader 99.33%
    Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models.
    Taragarestrant meglumine
  • HY-112596A
    H3B-6545 hydrochloride
    Antagonist 99.16%
    H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
    H3B-6545 hydrochloride
  • HY-145572A
    Imlunestrant tosylate
    Degrader 99.28%
    Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).
    Imlunestrant tosylate
  • HY-B0216S
    Ethynyl Estradiol-d4
    Agonist 99.00%
    Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Ethynyl Estradiol-d<sub>4</sub>
  • HY-141551
    GNE-274
    Degrader 98.00%
    GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
    GNE-274
  • HY-150693
    Estrogen receptor β antagonist 2
    Antagonist 98.39%
    Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively.
    Estrogen receptor β antagonist 2
  • HY-121149
    Droloxifene
    Modulator 99.89%
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
    Droloxifene
  • HY-W739985
    7α-(Thiomethyl)spironolactone
    Antagonist 98.76%
    7α-(Thiomethyl)spironolactone is a nuclear steroid receptor antagonist that can be used for the research of coronaviruses.
    7α-(Thiomethyl)spironolactone
  • HY-16023B
    (Rac)-Acolbifene
    Antagonist 98.18%
    (Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380.
    (Rac)-Acolbifene
  • HY-B0216R
    Ethinylestradiol (Standard)
    Agonist
    Ethynyl Estradiol (Standard) is the analytical standard of Ethynyl Estradiol. This product is intended for research and analytical applications.
    Ethinylestradiol (Standard)
  • HY-N2168
    Pinoresinol 4-O-β-D-glucopyranoside
    99.89%
    Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects.
    Pinoresinol 4-O-β-D-glucopyranoside
  • HY-103447R
    Zearalenone (Standard)
    Activator
    Zearalenone (Standard) is the analytical standard of Zearalenone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-138686
    GPR30 agonist-1
    Agonist 98.62%
    GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects.
    GPR30 agonist-1
  • HY-B0652
    Etonogestrel
    Agonist 99.91%
    Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel
  • HY-W011926
    Diisopropyl phthalate
    Ligand 99.37%
    Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM.
    Diisopropyl phthalate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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