2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR

Estrogen Receptor/ERR

Estrogen Receptor/ERR

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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.

Estrogen Receptor/ERR Isoform Specific Products:

Estrogen Receptor/ERR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-A0036R
    Bazedoxifene acetate (Standard)
    		Modulator
    Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
    Bazedoxifene acetate (Standard)
  • HY-B0141C
    Estradiol hemihydrate
    		Agonist 99.79%
    Estradiol (β-Estradiol) hemihydrate is a steroid hormone and the major female sex hormone. Estradiol (β-Estradiol) hemihydrate can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol (β-Estradiol) hemihydrate can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering.
    Estradiol hemihydrate
  • HY-N0570R
    Hydroxytyrosol (Standard)
    		Activator
    Hydroxytyrosol (Standard) (DOPET (Standard)) is the analytical standard of Hydroxytyrosol (HY-N0570). This product is intended for research and analytical applications. Hydroxytyrosol is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields.
    Hydroxytyrosol (Standard)
  • HY-W014798
    4,4'-Oxydiphenol
    		99.98%
    4,4'-Oxydiphenol (4,4'-Dihydroxydiphenyl ether) is an inhibitor of estrogen receptor (IC50 = 60 μM ) .
    4,4'-Oxydiphenol
  • HY-B0463R
    Clomiphene citrate (Standard)
    		Modulator
    Clomiphene (citrate) (Standard) is the analytical standard of Clomiphene (citrate). This product is intended for research and analytical applications. Clomiphene citrate (Clomifene citrate) is an orally active estrogen-receptor modulator. Clomiphene citrate has anti-cancer actixity, induces perturbations during meiotic maturation and cytogenetic abnormalities and ameliorates in managing psychiatric and cognitive impairment.
    Clomiphene citrate (Standard)
  • HY-101119
    GLL398
    		Degrader
    GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
    GLL398
  • HY-128838A
    (rel)-PROTAC ERRα Degrader-1
    		98.18%
    (rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
    (rel)-PROTAC ERRα Degrader-1
  • HY-18719C
    Endoxifen E-isomer hydrochloride
    		Inhibitor 98.20%
    Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects.
    Endoxifen E-isomer hydrochloride
  • HY-132194
    ERα degrader-2
    		Inhibitor 98.30%
    ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research.
    ERα degrader-2
  • HY-125263
    OP-1074
    		Degrader 99.77%
    OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
    OP-1074
  • HY-129619
    SNIPER(ER)-87
    		Modulator 99.2%
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
    SNIPER(ER)-87
  • HY-173178
    LNS8801
    		Agonist
    LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes.
    LNS8801
  • HY-N0587R
    Demethylzeylasteral (Standard)
    		Modulator
    Demethylzeylasteral (Standard) is the analytical standard of Demethylzeylasteral. This product is intended for research and analytical applications. Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation .
    Demethylzeylasteral (Standard)
  • HY-B1617AS
    Zuclomiphene-d4 citrate
    		Modulator 99.0%
    Zuclomiphene-d4 citrate is a deuterium labeled Zuclomiphene citrate (HY-B1617A). Zuclomiphene citrate is a cis isomer of Clomiphene citrate (HY-B0463). Zuclomiphene citrate is orally active and has an antiestrogenic effect. Zuclomiphene can reduce cholesterol levels. Zuclomiphene citrate can be for the researches of endocrinology and metabolic disease.
    Zuclomiphene-d<sub>4</sub> citrate
  • HY-116896A
    LY117018 TFA
    		Modulator 99.18%
    LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines.
    LY117018 TFA
  • HY-201580
    ER ligand-8
    ER ligand-8 is an ER (Estrogen Receptor/ERR) ligand that can be used to synthesize the PROTAC molecule ERD-1233 (HY-169367).
    ER ligand-8
  • HY-B0234S
    Estrone-13C3
    		Agonist 98.0%
    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.
    Estrone-<sup>13</sup>C<sub>3</sub>
  • HY-132247A
    (±)-ErSO
    		Control
    (±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator.
    (±)-ErSO
  • HY-B0390S
    Mestranol-d2
    		Agonist 99.0%
    Mestranol-d2 is the deuterium labeled Mestranol. Mestranol is an inactive proagent and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders. Mestranol-d2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mestranol-d<sub>2</sub>
  • HY-135585
    LY88074
    		Modulator 99.96%
    LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.
    LY88074
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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