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-121149B
    (E/Z)-Droloxifene
    Modulator
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity.
    (E/Z)-Droloxifene
  • HY-A0031S2
    Bazedoxifene-d4 acetate
    Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. 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[2][3].
    Bazedoxifene-d<sub>4</sub> acetate
  • HY-162220
    HSD17B13-IN-94
    Inhibitor
    HSD17B13-IN-94 (Compound 12) is an effective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤ 0.1 μM for Estradiol (HY-B0141). HSD17B13-IN-94 can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD, NASH, or drug-induced liver injury (DILI).
    HSD17B13-IN-94
  • HY-163812
    ER degrader 9
    Inhibitor
    ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer.
    ER degrader 9
  • HY-149500
    CITFA
    Agonist
    CITFA is a GPER agonist. CITFA can promote neurite growth of hippocampal neurons in rat embryo (E18).
    CITFA
  • HY-150601
    Estrogen receptor-IN-1
    Inhibitor 99.87%
    Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively.
    Estrogen receptor-IN-1
  • HY-144204
    Estrogen receptor antagonist 5
    Antagonist
    Estrogen receptor antagonist 5 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 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165).
    Estrogen receptor antagonist 5
  • HY-13738S4
    Raloxifene-d10-1
    Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. 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[2].
    Raloxifene-d<sub>10</sub>-1
  • HY-144314
    PSDalpha
    Inhibitor
    PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm.
    PSDalpha
  • HY-P99951
    Ripafollitropin alfa (bovine)
    Ripafollitropin alfa (bovine) is a recombinant follicle-stimulating hormone fusion protein with chorionic gonadotropin.
    Ripafollitropin alfa (bovine)
  • HY-18719ER
    Endoxifen (Standard)
    Methicillin (sodium hydrate) (Standard) is the analytical standard of Methicillin (sodium hydrate). This product is intended for research and analytical applications. Methicillin sodium hydrate is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin sodium hydrate is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins. Methicillin sodium hydrate can be used for the research of skin infections, osteomyelitis, and endocarditis.
    Endoxifen (Standard)
  • HY-N11438
    3'-Hydroxymirificin
    Inhibitor
    3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells.
    3'-Hydroxymirificin
  • HY-13636A
    Fulvestrant (S enantiomer)
    Fulvestrant S enantiomer (ICI 182780 S enantiomer) is the S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
    Fulvestrant (S enantiomer)
  • 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-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-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[1].
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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