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-B2158R
    Chlorotrianisene (Standard)
    Modulator
    Chlorotrianisene (Standard) is the analytical standard of Chlorotrianisene. This product is intended for research and analytical applications. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
    Chlorotrianisene (Standard)
  • HY-W326021
    Phenolphthalol
    Activator
    Phenolphthalol is a laxative in agent preparations and also estrogenically active.
    Phenolphthalol
  • HY-116939
    (E)-Broparestrol
    Activator
    (E)-Broparestrol is a biologically active tetrasubstituted olefin, which is used as an estrogen in dermatology.
    (E)-Broparestrol
  • HY-100583AR
    (±)-Equol (Standard)
    (±)-Equol (Standard) is the analytical standard of (±)-Equol. This product is intended for research and analytical applications. (±)-Equol is the racemate of equol. (±)-equol exhibits EC50s of 200 and 74 nM for human ERα and ERβ, respectively. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
    (±)-Equol (Standard)
  • HY-W615671
    4,4'-(Cyclohexylidenemethylene)diphenol
    Ligand
    4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetric cyclic nonsteroidal estrogen. 4,4'-(Cyclohexylidenemethylene)diphenol has high binding affinity for estrogen receptors ERα and ERβ.
    4,4'-(Cyclohexylidenemethylene)diphenol
  • HY-100689R
    Propyl pyrazole triol (Standard)
    Agonist
    Propyl pyrazole triol (Standard) is the analytical standard of Propyl pyrazole triol. This product is intended for research and analytical applications. Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%)[1][2].
    Propyl pyrazole triol (Standard)
  • HY-N15336
    Tschimganin
    Tschimganin is an ester of terpenoid acids with estrogen activity, which is found in F. tschimganica. Tschimganin can increase the growth of uterus of immature rats.
    Tschimganin
  • HY-A0036R
    Bazedoxifene (acetate) (Standard)
    Modulator
    Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
    Bazedoxifene (acetate) (Standard)
  • HY-A0031R
    Bazedoxifene (Standard)
    Modulator
    Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
    Bazedoxifene (Standard)
  • HY-N2168R
    Pinoresinol 4-O-β-D-glucopyranoside (Standard)
    Pinoresinol 4-O-β-D-glucopyranoside (Standard) is the analytical standard of Pinoresinol 4-O-β-D-glucopyranoside (HY-N2168). This product is intended for research and analytical applications. 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 (Standard)
  • 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[1].
    Clomiphene-d<sub>5</sub> citrate
  • 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>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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