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-103447R
    Zearalenone (Standard)
    		Activator
    Zearalenone (Standard) is the analytical standard of Zearalenone. This product is intended for research and analytical applications. Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts.
    Zearalenone (Standard)
  • HY-138686
    GPR30 agonist-1
    		Agonist 98.62%
    GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects.
    GPR30 agonist-1
  • HY-N2026S1
    Propylparaben-d4
    		Agonist 99.55%
    Propylparaben-d4 (Propyl parahydroxybenzoate-d4) is the deuterium labeled Propylparaben (HY-N2026). Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is an orally active weak estrogen receptor agonist. Propylparaben regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
    Propylparaben-d<sub>4</sub>
  • HY-13636S
    Fulvestrant-d3
    		Antagonist
    Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
    Fulvestrant-d<sub>3</sub>
  • HY-135309
    PROTAC ER Degrader-4
    		Inhibitor 98.78%
    PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
    PROTAC ER Degrader-4
  • HY-159613
    PELP1-IN-1
    		Inhibitor 99.28%
    PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER+ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer.
    PELP1-IN-1
  • HY-W009300S
    4-Hydroxyestrone-d4
    		99.35%
    4-Hydroxyestrone (4-OHE1)-d4 is the deuterium 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-d<sub>4</sub>
  • HY-B0412S2
    Estriol-d3
    		Antagonist
    Estriol-d3 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
    Estriol-d<sub>3</sub>
  • HY-113251S
    2-Hydroxyestrone-d4
    		Inhibitor
    2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
    2-Hydroxyestrone-d<sub>4</sub>
  • HY-P5464
    SRC-1 NR box peptide
    		98.18%
    SRC-1 NR box peptide is a biological active peptide (This peptide is a 14-amino acid fragment from the steroid receptor cofactor SRC-1 NR II). SRC-1 NR box peptide can be used to study the regulatory mechanisms of estrogen receptor ligands.
    SRC-1 NR box peptide
  • HY-A0036B
    Bazedoxifene acetate-B
    Bazedoxifene (acetate)-B (TSE-424 (acetate)-B) is the B-crystal form compound of Bazedoxifene acetate (HY-A0036).
    Bazedoxifene acetate-B
  • HY-N0322S4
    Cholesterol-13C3
    		Agonist 98.80%
    Cholesterol-13C3 is the 13C-labeled Cholesterol. 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-<sup>13</sup>C<sub>3</sub>
  • HY-126109
    (±)-8-Prenylnaringenin
    		Modulator 99.97%
    (±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogen receptor modulator (SERM) (Estrogen Receptor/ERR) that inhibits ERα and ERβ with IC50s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research.
    (±)-8-Prenylnaringenin
  • HY-145556
    Bexirestrant
    		Inhibitor 99.46%
    Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.
    Bexirestrant
  • HY-B1830
    Estradiol enanthate
    		98.07%
    Estradiol enanthate (E2EN) is a shorter-acting estrogen. Estradiol enanthate is an injectable contraceptive in combination with Dihydroxyprogesterone acetophenide. Estradiol enanthate promotes withdrawal bleeding, in a pattern similar to menstruation.
    Estradiol enanthate
  • HY-N6043
    Hydroxytyrosol acetate
    		Activator 98.10%
    Hydroxytyrosol acetate is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol acetate not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol acetate effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol acetate 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 acetate has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields.
    Hydroxytyrosol acetate
  • HY-161740
    PHTPP-1304
    		Degrader 99.96%
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.
    PHTPP-1304
  • HY-137818
    SR19881
    		Agonist 99.30%
    SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively.
    SR19881
  • HY-124414
    4'-Hydroxytamoxifen
    		Modulator 99.2%
    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
  • HY-B0316R
    Avobenzone (Standard)
    		Antagonist
    Avobenzone (Standard) is the analytical standard of Avobenzone. This product is intended for research and analytical applications. 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.
    Avobenzone (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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