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-B0141S4
    Estradiol-13C6
    Agonist
    Estradiol-13C6 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
    Estradiol-<sup>13</sup>C<sub>6</sub>
  • HY-16950AR
    (E/Z)-4-Hydroxytamoxifen (Standard)
    Modulator
    (E/Z)-4-Hydroxytamoxifen (Standard) is the analytical standard of (E/Z)-4-Hydroxytamoxifen. This product is intended for research and analytical applications. (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity.
    (E/Z)-4-Hydroxytamoxifen (Standard)
  • HY-18295A
    rel-Erteberel
    Agonist
    rel-Erteberel is rel isomer of Erteberel (HY-18295). Erteberel is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities.
    rel-Erteberel
  • HY-B0652R
    Etonogestrel (Standard)
    Agonist
    Etonogestrel (Standard) is the analytical standard of Etonogestrel. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B1830R
    Estradiol enanthate (Standard)
    Estradiol enanthate (Standard) is the analytical standard of Estradiol enanthate. Estradiol enanthate (E2EN) is a shorter-acting estrogen. Estradiol enanthate is an injectable contraceptive in combination with Dihydroxyprogesterone acetophenide. Estradiol enanthate promotes withdrawal bleeding, in a pattern similar to menstruation.
    Estradiol enanthate (Standard)
  • HY-B0652S1
    Etonogestrel-d6
    Agonist
    Etonogestrel-d6 is deuterium labeled Etonogestrel. 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-d<sub>6</sub>
  • HY-155196
    ER degrader 6
    Degrader
    ER degrader 6 (compound 35s) is a potent Estrogen Receptor (ER)α degrader. ER degrader 6 disrupts the microtubule network by restraining tubulin polymerization. ER degrader 6 suppresses tumor growth without noticeable poisonousness.
    ER degrader 6
  • HY-B1403S1
    E,E-Dienestrol-d6-1
    Agonist
    E,E-Dienestrol-d6-1 is a deuterated labeled Dienestrol.
    E,E-Dienestrol-d<sub>6</sub>-1
  • HY-121198
    Dimestrol
    Dimestrol (Diethylstilbestrol dimethyl ether) is a precursor of Diethylstilbestrol (HY-14598).
    Dimestrol
  • HY-13556
    Arzoxifene
    Modulator
    Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
    Arzoxifene
  • HY-N3755R
    Dihydroresveratrol (Standard)
    Modulator
    Clofarabine (Standard) is the analytical standard of Clofarabine. This product is intended for research and analytical applications. Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit.
    Dihydroresveratrol (Standard)
  • HY-W040046
    Nafoxidine hydrochloride
    Antagonist
    Nafoxidine hydrochloride is a non-steroidal estrogen receptor antagonist with antitumor activity for breast cancer.
    Nafoxidine hydrochloride
  • HY-122359
    Levormeloxifene
    Modulator
    Levormeloxifene (L-Centchroman) is a selective estrogen receptor modulator (SERM), which prevents and ameliorates postmenopausal osteoporosis. Levormeloxifene causes multiple adverse gynecological effects.
    Levormeloxifene
  • HY-172231
    Hexolame
    Agonist
    Hexolame is an estrogen receptors agonist with dual anticoagulant and estrogenic properties. Hexolame binds to estrogen receptors to induce anticoagulant effects by modulating clotting factors or platelet activity. Hexolame is promising for research of prostatic cancer and prevention of thrombosis.
    Hexolame
  • HY-B1617
    Zuclomiphene
    Modulator
    Zuclomiphene is a cis isomer of Clomiphene citrate (HY-B0463). Zuclomiphene is orally active and has an antiestrogenic effect. Zuclomiphene can reduce cholesterol levels. Zuclomiphene can be for the researches of endocrinology and metabolic disease.
    Zuclomiphene
  • HY-103451A
    rel-(R,R)-THC
    Antagonist
    rel-(R,R)-THC is the relative configuration of (R,R)-THC (HY-103451). (R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6.
    rel-(R,R)-THC
  • HY-149970
    ER degrader 5
    Degrader
    ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer.
    ER degrader 5
  • HY-19822S
    Elacestrant-d4
    Inhibitor
    Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER+ breast cancer cell lines both in vitro and in vivo.
    Elacestrant-d<sub>4</sub>
  • HY-N0250R
    Saikosaponin D (Standard)
    Activator
    Saikosaponin D (Standard) is the analytical standard of Saikosaponin D. This product is intended for research and analytical applications. Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
    Saikosaponin D (Standard)
  • HY-B1403S
    Dienestrol-d2
    Agonist
    Dienestrol-d2 is a deuterium labeled Dienestrol (HY-B1403).
    Dienestrol-d<sub>2</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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