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-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-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[1][2][3][4].
    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
  • HY-B1623
    Cyproterone
    99.89%
    Cyproterone is an antiandrogen that suppresses the actions of testosterone via blocking androgen receptors. Cyproterone’s acetate form can be used in the research of hypersexuality and prostate cancer.
    Cyproterone
  • HY-201580
    ER ligand-8
    ER ligand-8 is an ER (Estrogen Receptor/ERR) ligand that can be used to synthesize the PROTAC molecule ERD-1233 (HY-169367).
    ER ligand-8
  • HY-132247B
    (S)-ErSO
    Control 99.40%
    (S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105).
    (S)-ErSO
  • HY-132247A
    (±)-ErSO
    Control
    (±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator.
    (±)-ErSO
  • HY-W1006471
    Estrogen receptor-agonist-1
    Agonist
    Estrogen receptor-agonist-1 (compound 4e) is a estrogen receptor (ER) agonist that binds to ERα with high affinity.
    Estrogen receptor-agonist-1
  • HY-B0390S
    Mestranol-d2
    Agonist ≥99.0%
    Mestranol-d2 is the deuterium labeled Mestranol. Mestranol is an inactive proagent and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders[1][2][3]. Mestranol-d2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mestranol-d<sub>2</sub>
  • HY-N2448
    Lindleyin
    Activator 99.95%
    Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors. Lindleyin binds to ERα with estrogenic activity.
    Lindleyin
  • HY-135585
    LY88074
    Modulator 99.96%
    LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.
    LY88074
  • HY-137004
    Indazole-Cl
    Agonist 98.72%
    Indazole-Cl (Ind-Cl) is an Estrogen receptor (ER)-β-specific agonist with inflammatory effect. Indazole-Cl inhibits cyclooxygenase-2 exression reduction induced by hypoxia. And Indazole-Cl inhibits ROS production. Indazole-Cl also inhibits cell migration and invasion by hypoxia increased by hypoxia. Indazole-Cl is potent inhibitor of hypoxia-induced inflammation in vascular smooth muscle cells (VSMCs).
    Indazole-Cl
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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