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-179045
    ERα degrader 14
    Degrader
    ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer.
    ERα degrader 14
  • HY-138690
    Estrogen receptor modulator 6
    Agonist
    Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (Ki=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(Ki=8.4 nM).
    Estrogen receptor modulator 6
  • HY-144206
    Estrogen receptor antagonist 6
    Antagonist
    Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166).
    Estrogen receptor antagonist 6
  • HY-N15700
    Toralactone 9-O-triglucoside
    Toralactone 9-O-triglucoside (Compound 2) is a phenolic trisaccharide. Toralactone 9-O-triglucoside can be isolated from Cassia seed. Toralactone 9-O-triglucoside can be used in the research of estrogen-related diseases such as breast cancer, prostate cancer, osteoporosis and cardiovascular disease.
    Toralactone 9-O-triglucoside
  • HY-143253
    Estrogen receptor antagonist 7
    Antagonist
    Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities.
    Estrogen receptor antagonist 7
  • HY-149969
    ER degrader 4
    Degrader
    ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity.
    ER degrader 4
  • HY-174870
    PROTAC ERα Degrader-11
    Degrader
    PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)).
    PROTAC ERα Degrader-11
  • HY-135596
    Raloxifene dimethyl ester hydrochloride
    Control
    Raloxifene dimethyl ester hydrochloride is an analog of Raloxifene, extracted from patent US5464845A, compound 28.
    Raloxifene dimethyl ester hydrochloride
  • HY-13738S3
    Raloxifene-d10
    Modulator
    Raloxifene-d10 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>10</sub>
  • HY-168869
    Tamoxifen-PEG-Clozapine
    Degrader
    Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer. (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))
    Tamoxifen-PEG-Clozapine
  • HY-122359A
    rel-Levormeloxifene
    Modulator
    rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells.
    rel-Levormeloxifene
  • HY-B1630
    Stilbestrol dipropionate
    Stilbestrol dipropionate is an estrogen-like compound with hormone suppressive activity for recurrent prostate cancer. Stilbestrol dipropionate can be used to suppress diseases associated with estrogen deficiency.
    Stilbestrol dipropionate
  • HY-168270
    PROTAC ER Degrader-11
    Degrader
    PROTAC ER Degrader-11 (Example 26-1) is a potent PROTAC ER degrader, with the IC50 of 0.66 nM. PROTAC ER Degrader-11 plays an important role in cancer research(Sturcture Note:(Blue: Cereblon ligand (HY-W797329), Black: linker (HY-W262798);Pink: ER ligand (HY-168271)).
    PROTAC ER Degrader-11
  • HY-W100026S
    Galaxolide-d6 (mixture of diastereomers) (>80%)
    Galaxolide-d6 (mixture of diastereomers) (>80%) is the deuterium labeled Galaxolide (HY-W100026). Galaxolide can induce estrogenic activity (Estrogen Receptor/ERR), trigger oxidative stress and genotoxicity, and induce EROD and GST (Glutathione S-transferase) enzyme activity.
    Galaxolide-d<sub>6</sub> (mixture of diastereomers) (>80%)
  • HY-155492
    ERα degrader 7
    Degrader
    ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research.
    ERα degrader 7
  • HY-15731S1
    Estetrol-d4 (Major)
    Estetrol-d4 (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research.
    Estetrol-d<sub>4</sub> (Major)
  • HY-122411
    Panomifene
    Inhibitor
    Panomifene (EGIS 5650) is a tamoxifen (HY-13757A) analog with an antiestrogenic activity. Panomifene can be used in the research of breast cancer.
    Panomifene
  • HY-103453
    (R)-DPN
    Chemical
    (R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively.
    (R)-DPN
  • HY-103452
    RU58668
    Antagonist
    RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research.
    RU58668
  • HY-135582
    Raloxifene 4'-glucuronide
    Modulator
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective 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 4'-glucuronide
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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