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-B1176S
    Equilin-d4
    Agonist
    Equilin-d4 is the deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism[1][2].
    Equilin-d<sub>4</sub>
  • 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-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
  • HY-18719BR
    Endoxifen hydrochloride (Standard)
    Inhibitor
    Endoxifen (hydrochloride) (Standard) is the analytical standard of Endoxifen (hydrochloride). This product is intended for research and analytical applications. Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study[1][2].
    Endoxifen hydrochloride (Standard)
  • HY-103446
    FERb 033
    Agonist
    FERb 033 is a selective and potent ERβ agonist (Ki=7.1 nM, EC50=4.8 nM). FERb 033 shows 62-fold selectivity over ERα.
    FERb 033
  • HY-118950
    J 628
    J 628 is an estrogen derivative used to study antifertility effects after sexual intercourse in mice, rats, and rabbits.
    J 628
  • HY-B1623
    Cyproterone
    Cyproterone is an antiandrogen that suppresses the actions of testosterone via blocking androgen receptors. Cyproterone’s acetate form can be used in the research of hypersexuality and prostate cancer.
    Cyproterone
  • HY-117649
    RU-39411
    RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen.
    RU-39411
  • HY-118861B
    Enclomiphene hydrochloride
    Antagonist
    Enclomiphene ((E)-Clomiphene) hydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene hydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
    Enclomiphene hydrochloride
  • HY-170334
    ER ligand-7
    Ligand
    ER ligand-7 is the ligand for estrogen receptor, and can be used for synthesis of PROTAC ER Degrader-15 (HY-170332) as ligand for target protein.
    ER ligand-7
  • HY-B0234S
    Estrone-13C3
    Agonist
    Estrone-13C3 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
    Estrone-<sup>13</sup>C<sub>3</sub>
  • HY-137391
    2-Bromoestradiol
    Inhibitor
    2-Bromoestradiol is a estrogen 2-hydroxylase inhibitor. 2-Bromoestradiol decreases irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins.
    2-Bromoestradiol
  • HY-163680
    ERα degrader 9
    ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679).
    ERα degrader 9
  • HY-B0316S
    Avobenzone-13C,d3
    Antagonist
    Avobenzone-13C,d3 is the 13C- and deuterium labeled Avobenzone. Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist[1][2].
    Avobenzone-<sup>13</sup>C,d<sub>3</sub>
  • HY-144306
    ERα degrader 4
    ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer.
    ERα degrader 4
  • HY-124414R
    4'-Hydroxytamoxifen (Standard)
    Modulator
    4'-Hydroxytamoxifen (Standard) is the analytical standard of 4'-Hydroxytamoxifen. This product is intended for research and analytical applications. 4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells.
    4'-Hydroxytamoxifen (Standard)
  • HY-135594
    4'-Raloxifene-β-D-glucopyranoside
    Antagonist
    4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
    4'-Raloxifene-β-D-glucopyranoside
  • HY-135581S1
    Raloxifene 6-glucuronide-d4 lithium
    Modulator
    Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. 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[1][2][3].
    Raloxifene 6-glucuronide-d<sub>4</sub> lithium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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