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-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)
  • HY-W011927R
    4,4'-Sulfonyldiphenol (Standard)
    Antagonist
    4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
    4,4'-Sulfonyldiphenol (Standard)
  • HY-N6709
    Zeranol
    Agonist 98.82%
    Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
    Zeranol
  • HY-B1192R
    Estradiol benzoate (Standard)
    Agonist
    Estradiol benzoate (Standard) is the analytical standard of Estradiol benzoate. This product is intended for research and analytical applications. Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice.
    Estradiol benzoate (Standard)
  • HY-14598R
    Diethylstilbestrol (Standard)
    Agonist
    Diethylstilbestrol (Standard) is the analytical standard of Diethylstilbestrol. This product is intended for research and analytical applications. Diethylstilbestrol (Stilbestrol) is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor..
    Diethylstilbestrol (Standard)
  • HY-W011926
    Diisopropyl phthalate
    Ligand 99.37%
    Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM.
    Diisopropyl phthalate
  • HY-112098
    PROTAC ERα Degrader-1
    Inhibitor
    PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
    PROTAC ERα Degrader-1
  • HY-126351
    PROTAC ERRα ligand 2
    Antagonist 99.36%
    PROTAC ERRα ligand 2 is a ERRα ligand with a target IC50 of 5.67 nM. PROTAC ERRα ligand 2 blocks the protein-protein interaction between ERRα and PGC-1α. PROTAC ERRα ligand 2 can be used for synthesis of PROTACs.
    PROTAC ERRα ligand 2
  • HY-N0322S7
    Cholesterol-d1
    Agonist 99.29%
    Cholesterol-d1 is the deuterium 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-d<sub>1</sub>
  • HY-128838
    PROTAC ERRα Degrader-1
    Inhibitor 98.22%
    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 PROTAC estrogen-related receptor alpha (ERRa) degrader.
    PROTAC ERRα Degrader-1
  • HY-103457
    Y134
    Antagonist 99.67%
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.
    Y134
  • HY-B0141S3
    Estradiol-d2
    Agonist 98.03%
    Estradiol-d2 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
    Estradiol-d<sub>2</sub>
  • HY-118860
    Corifollitropin alfa
    Agonist
    Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility.
    Corifollitropin alfa
  • HY-N0570S
    Hydroxytyrosol-d4
    Activator
    Hydroxytyrosol-d4 (DOPET-d4) is the deuterium labeled Hydroxytyrosol (HY-N0570). 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-d<sub>4</sub>
  • HY-B0487
    Ethisterone
    Agonist 98.02%
    Ethisterone (Pregneninolone; 17α-Ethynyltestosterone) is a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone has almost no effect on the phagocytic activity of the reticuloendothelial system in male guinea pigs, while in utero exposure can induce abnormalities in the urogenital system of offspring.
    Ethisterone
  • HY-137391
    2-Bromoestradiol
    Inhibitor 99.59%
    2-Bromoestradiol is a estrogen 2-hydroxylase inhibitor. 2-Bromoestradiol decreases irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins.
    2-Bromoestradiol
  • HY-111061
    GTX-758
    Agonist 99.59%
    GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research.
    GTX-758
  • HY-150693
    Estrogen receptor β antagonist 2
    Antagonist 98.39%
    Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively.
    Estrogen receptor β antagonist 2
  • HY-N2448
    Lindleyin
    Activator 99.95%
    Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors. Lindleyin binds to ERα with estrogenic activity.
    Lindleyin
  • HY-110157
    AC-186
    Agonist 99.61%
    AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease.
    AC-186
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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