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-B1662S
    (Rac)-Hexestrol-d4
    (Rac)-Hexestrol-d4 is the deuterium labeled (Rac)-Hexestrol.
    (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 98.61%
    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.
    Raloxifene-d<sub>4</sub> hydrochloride
  • HY-B1662S1
    (Rac)-Hexestrol-d6
    (Rac)-Hexestrol-d6 is the deuterium labeled (Rac)-Hexestrol.
    (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-N17632
    Moracin G
    Inhibitor
    Moracin G is a plant-derived kinase modulator and receptor ligand that forms stable bindings with multiple key proteins (AKT1, COX2 and Estrogen receptor 1) and competitively inhibits the activity of specific kinases. By binding to MELK to disrupt cell cycle regulation, Moracin G impairs the survival and proliferation of cancer cells, induces cancer cell apoptosis, and thereby exerts anti-tumor potential. Moracin G can be used in research related to periodontitis and breast cancer.
    Moracin G
  • 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 (HY-B1617A). Zuclomiphene citrate is a cis isomer of Clomiphene citrate (HY-B0463). Zuclomiphene citrate is orally active and has an antiestrogenic effect. Zuclomiphene can reduce cholesterol levels. Zuclomiphene citrate can be for the researches of endocrinology and metabolic disease.
    Zuclomiphene-d<sub>5</sub> citrate
  • HY-125263B
    (R)-OP-1074
    Control 98.24%
    (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-W011926S
    Diisopropyl phthalate-d4
    Ligand 98.8%
    Diisopropyl phthalate-d4 (DiPP-d4) is the deuterium labeled Diisopropyl Phthalate (HY-W011926). 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-d<sub>4</sub>
  • HY-163467
    CHEMBL4224880
    Ligand
    CHEMBL4224880 is an estrogen receptor-α (ER-α) binder.
    CHEMBL4224880
  • HY-184011
    SERT-IN-4
    Agonist
    SERT-IN-4 is a brain-penetrant and orally active SERT inhibitor and ERβ agonist with human SERT IC50 of 16.92 nM and human ERβ EC50 of 3.66 nM. SERT-IN-4 inhibits SERT-mediated substrate transport, increases hippocampal serotonin levels, modulates p-CREB and BDNF expression.SERT-IN-4 reduces immobility in CUMS mice, improves social interaction and reduces inactivity in CSDS mice.SERT-IN-4 can be used for the research of major depressive disorder.
    SERT-IN-4
  • HY-174131
    PVTX-321
    Degrader
    PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer.
    PVTX-321
  • HY-175171
    Anticancer agent 276
    Inhibitor
    Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.
    Anticancer agent 276
  • 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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