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-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-174338
    GPER/Bcl-2-IN-1
    Inhibitor
    GPER/Bcl-2-IN-1 is a GPER/Bcl-2 inhibitor. GPER/Bcl-2-IN-1 can inhibit the proliferation and neurospheres formation of glioblastoma cells. GPER/Bcl-2-IN-1 can be used for the study of glioblastoma multiforme (GBM).
    GPER/Bcl-2-IN-1
  • HY-149500
    CITFA
    Agonist
    CITFA is a GPER agonist. CITFA can promote neurite growth of hippocampal neurons in rat embryo (E18).
    CITFA
  • HY-N0322GL
    Cholesterol (GMP Like)
    Agonist
    Cholesterol (GMP Like) is Cholesterol (HY-N0322) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
    Cholesterol (GMP Like)
  • HY-179238
    CS-1-103
    Inhibitor
    CS-1-103 is a potent estrogen receptor (ER) inhibitor. CS-1-103 inhibits ER transcriptional activity with an EC50 of 0.36 μM by recruiting methyl-CpG binding domain protein 2 (MBD2), HDACs and the nucleosome remodeling and deacetylase (NuRD) complex. CS-1-103 can be used for breast and prostate cancer research.
    CS-1-103
  • 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-176225
    BY13
    Inhibitor
    BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model. Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
    BY13
  • HY-128528
    PROTAC ER Degrader-2
    Inhibitor
    PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    PROTAC ER Degrader-2
  • HY-W744272
    Estetrol-d3
    Estetrol-d3 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>3</sub>
  • 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-W009300S1
    4-Hydroxyestrone-13C6
    4-Hydroxyestrone (4-OHE1)-13C6 is a 13C-labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease.
    4-Hydroxyestrone-<sup>13</sup>C<sub>6</sub>
  • 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-180961
    His-TERRα
    Degrader
    His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer.
    His-TERRα
  • 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-W701943
    Fenhexamid-d10
    Fenhexamid-d10 is the deuterium labeled Fenhexamid (HY-118065). Fenhexamid, a botryticide, is a sterol biosynthesis inhibitor. Fenhexamid shows fungicide efficient against the plant pathogenic fungus Botryotinia fuckeliana (Botrytis cinerea).
    Fenhexamid-d<sub>10</sub>
  • HY-179597
    ERα ligand 3
    ERα ligand 3 is a PROTAC target protein ligand that targets ERα. ERα ligand 3 can be used for the synthesis of CV2a (HY-179576).
    ERα ligand 3
  • 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
Cat. No. Product Name / Synonyms Species Source
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