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-153478
    Estrogen receptor modulator 7
    Modulator
    Estrogen receptor modulator 7 is a potent estrogen receptor modulator. Estrogen receptor modulator 7 can be used in research of cancer.
    Estrogen receptor modulator 7
  • HY-142926
    ER degrader 2
    ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1).
    ER degrader 2
  • HY-169063
    ZINC05925939
    Inhibitor
    ZINC05925939 is an estrogen receptor beta (ESR2) inhibitor that can be used in breast cancer research.
    ZINC05925939
  • HY-171791
    WAY-166818
    Agonist
    WAY-166818 (WAY-818) is a synthetic nonsteroidal estrogen that is a selective agonist of ERβ.
    WAY-166818
  • HY-B0005AS
    Toremifene-d6
    Modulator
    Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively.
    Toremifene-d<sub>6</sub>
  • HY-14598S1
    Diethylstilbestrol-d3
    Agonist
    Diethylstilbestrol-d3 is deuterium labeled Diethylstilbestrol.
    Diethylstilbestrol-d<sub>3</sub>
  • HY-N8170
    4',2-Dihydroxy-4,6-dimethoxydihydrochalcone
    Agonist
    4',2-Dihydroxy-4,6-dimethoxydihydrochalcone, an estrogen agonist, shows binding affinity for bovine uterine estrogen receptor with an IC5050 of 15 μM.
    4',2-Dihydroxy-4,6-dimethoxydihydrochalcone
  • HY-167701
    OBHSA
    Degrader
    OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders.
    OBHSA
  • HY-120207
    (R)-GDC-0927
    Antagonist 98.78%
    (R)-GDC-0927 ((R)-SRN-927) is a (R)-enantiomer of GDC-0927 (HY-111484).
    (R)-GDC-0927
  • HY-118861
    Enclomiphene
    Antagonist
    Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
    Enclomiphene
  • HY-W727814
    Pipendoxifene-d10
    Pipendoxifene-d10 (ERA-923-d10) is the deuterium labeled Pipendoxifene (HY-13724). Pipendoxifene is a selective estrogen receptor modulator (SERM).
    Pipendoxifene-d<sub>10</sub>
  • HY-172869
    Estrogen receptor modulator 13
    Antagonist
    Estrogen receptor modulator 13 (Compound 5D) is an estrogen receptor antagonist. Estrogen receptor modulator 13 shows significant cytotoxicity against MCF7 cells with an IC50 value of 8.50 μM. Estrogen receptor modulator 13 is promising for research of breast cancers.
    Estrogen receptor modulator 13
  • HY-N11787
    Cimicifuga racemosa extract
    Inhibitor
    Cimicifuga racemosa extract is a herbal remedy with antiestrogenic properties found in the plant Cimicifuga racemosa, commonly used to alleviate menopausal symptoms and relieve symptoms such as hot flashes and night sweats.
    Cimicifuga racemosa extract
  • HY-144137
    Estrogen receptor antagonist 1
    Antagonist
    Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4).
    Estrogen receptor antagonist 1
  • HY-168101
    ERα degrader 11
    Degrader
    ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells.
    ERα degrader 11
  • HY-129099AR
    N-Desmethyltamoxifen hydrochloride (Standard)
    Antagonist
    N-Desmethyltamoxifen (hydrochloride) (Standard) is the analytical standard of N-Desmethyltamoxifen (hydrochloride). This product is intended for research and analytical applications. N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].
    N-Desmethyltamoxifen hydrochloride (Standard)
  • HY-170806
    ERα degrader 12
    Degrader
    ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model.
    ERα degrader 12
  • HY-172067
    ER ligand-9
    ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor/ERR) and a linker, which can be used to synthesize PROTAC ERD-1233 (HY-169367).
    ER ligand-9
  • HY-W654296
    Octocrylene-13C3
    Octocrylene-13C3 is the 13C-labeled Octocrylene (HY-A0087). Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes.
    Octocrylene-<sup>13</sup>C<sub>3</sub>
  • HY-123163
    JNJ-1250132
    Inhibitor
    JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM).
    JNJ-1250132
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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