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-129619
    SNIPER(ER)-87
    Modulator
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
    SNIPER(ER)-87
  • HY-13738S
    Raloxifene-d4
    Modulator
    Raloxifene-d4 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
    Raloxifene-d<sub>4</sub>
  • HY-18719ES
    Endoxifen-d5
    Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study[1][2].
    Endoxifen-d<sub>5</sub>
  • HY-B1662S
    (Rac)-Hexestrol-d4
    (Rac)-Hexestrol-d4 is the deuterium labeled (Rac)-Hexestrol[1].
    (Rac)-Hexestrol-d<sub>4</sub>
  • HY-B0672S
    Estradiol valerianate-d9
    Agonist
    Estradiol valerianate-d9 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
    Estradiol valerianate-d<sub>9</sub>
  • HY-13738S2
    Raloxifene-d4 hydrochloride
    Modulator
    Raloxifene-d4 (hydrochloride) is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].
    Raloxifene-d<sub>4</sub> hydrochloride
  • HY-B1662S1
    (Rac)-Hexestrol-d6
    (Rac)-Hexestrol-d6 is the deuterium labeled (Rac)-Hexestrol[1].
    (Rac)-Hexestrol-d<sub>6</sub>
  • HY-155737
    ET receptor antagonist 1
    Inhibitor
    ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model.
    ET receptor antagonist 1
  • HY-121094
    Androgen receptor allosteric antagonist 1
    Antagonist
    Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer.
    Androgen receptor allosteric antagonist 1
  • HY-B0216S2
    Ethynyl Estradiol-13C2
    Agonist
    Ethynyl Estradiol-13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 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-<sup>13</sup>C<sub>2</sub>
  • 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-W926789
    (E)-GW7604
    Antagonist
    (E)-GW7604 is the (E)-isomer of GW7604, an antiestrogen and a metabolite of GW5638 (HY-112746), which is a high-affinity estrogen receptor (ER) antagonist.
    (E)-GW7604
  • HY-B1617AS1
    Zuclomiphene-d5 citrate
    Zuclomiphene-d5 (citrate) is the deuterium labeled Zuclomiphene citrate[1]. Zuclomiphene citrate is a cis isomer of Clomiphene 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[2][3][4][5].
    Zuclomiphene-d<sub>5</sub> citrate
  • HY-125263B
    (R)-OP-1074
    Control
    (R)-OP-1074 is an isomer of OP-1074 (HY-125263) and can serve as a control compound in experiments. OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
    (R)-OP-1074
  • HY-155739
    ET receptor antagonist 3
    Inhibitor
    ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model.
    ET receptor antagonist 3
  • HY-155738
    ET receptor antagonist 2
    Inhibitor
    ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model.
    ET receptor antagonist 2
  • HY-119418
    Desketoraloxifene
    Activator
    Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer.
    Desketoraloxifene
  • HY-163467
    CHEMBL4224880
    Ligand
    CHEMBL4224880 is an estrogen receptor-α (ER-α) binder.
    CHEMBL4224880
  • HY-135581
    Raloxifene 6-glucuronide
    Modulator
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
    Raloxifene 6-glucuronide
  • HY-146267
    ERα degrader 5
    Antagonist
    ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
    ERα degrader 5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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