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-13724
    Pipendoxifene
    		Modulator 99.93%
    Pipendoxifene is a selective estrogen receptor modulator (SERM).
    Pipendoxifene
  • HY-112596
    H3B-6545
    		Antagonist 99.44%
    H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
    H3B-6545
  • HY-128600
    ERD-308
    		Inhibitor 98.13%
    ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker：(HY-172645))
    ERD-308
  • HY-13724B
    Pipendoxifene hydrochloride
    		Modulator 99.83%
    Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer.
    Pipendoxifene hydrochloride
  • HY-N0322S1
    Cholesterol-d6
    		Agonist 99.0%
    Cholesterol-d6 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>6</sub>
  • HY-N0791
    Tectoridin
    		99.85%
    Tectoridin is a isoflavone isolated from Maackia amurensis. Tectoridin is a phytoestrogen and activates estrogen and thyroid hormone receptors. Tectoridin exerts the estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway.
    Tectoridin
  • HY-132247
    ErSO
    		Activator 99.95%
    ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.
    ErSO
  • HY-B0708
    β-Estradiol 17-acetate
    		Agonist 99.93%
    β-Estradiol 17-acetate (1,3,5(10)-Estratriene-3,17β-diol 17-acetate) is a long-acting endogenous estrogen precursor and also a cell viability and proliferation enhancer. β-Estradiol 17-acetate promotes the adhesion and proliferation of freshly isolated and revived female-derived human brain microvascular endothelial cells, and reverses the decreased viability of revived male-derived human brain microvascular endothelial cells. β-Estradiol 17-acetate exerts the microvascular protective effect of estrogen, enabling non-tumor human brain microvascular endothelial cells to be cultured in vitro for 2 months after cryopreservation. β-Estradiol 17-acetate is biotransformed into β-estradiol via hydrolase action in the in vitro skin of humans, hairless dogs, rats and hairless mice.
    β-Estradiol 17-acetate
  • HY-B1234
    Octinoxate
    		Modulator 99.84%
    Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate
  • HY-W013935
    Bisphenol B
    		Agonist 99.34%
    Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties.
    Bisphenol B
  • HY-W011927S
    4,4'-Sulfonyldiphenol-d8
    		Agonist 99.21%
    4,4'-Sulfonyldiphenol-d8 (Bisphenol S (4,4'-Sulfonyldiphenol)-d8) is the deuterium labeled 4,4'-Sulfonyldiphenol (HY-W011927).4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), 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-d<sub>8</sub>
  • HY-133017
    Amcenestrant
    		Degrader 99.79%
    SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER+ breast cancer.
    Amcenestrant
  • HY-18719B
    Endoxifen hydrochloride
    		Inhibitor 98.04%
    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.
    Endoxifen hydrochloride
  • HY-N0910
    Notoginsenoside Ft1
    		Activator 99.49%
    Notoginsenoside Ft1 is an orally active bioactive saponin. Notoginsenoside Ft1 inhibits the PI3K/AKT/mTOR signaling pathway, activates the p38 MAPK and ERK1/2 signaling pathways, and increases the proportion of CD8+ T cells, thereby inducing apoptosis and lysosomal cell death in various cancer cells, and promoting angiogenesis. Notoginsenoside Ft1 causes vasodilation by activating glucocorticoid receptors (GR) and estrogen receptor beta (ERβ) in endothelial cells. Notoginsenoside Ft1 increases intracellular Ca2+ accumulation, reduces cAMP levels by activating a signaling network mediated through P2Y12 receptors, and promotes platelet aggregation, thereby exerting a procoagulant effect. Notoginsenoside Ft1 inhibits ferroptosis (ferroptosis) in renal tubular epithelial cells by activating the TGR5 receptor, thereby demonstrating a renal protective effect. Notoginsenoside Ft1 acts as a TGR5 agonist and an FXR antagonist to combat obesity and insulin resistance.
    Notoginsenoside Ft1
  • HY-B0316
    Avobenzone
    		Antagonist 98.0%
    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
  • HY-121528
    Nilestriol
    		98.93%
    Nilestriol is a estriol derivative, which inhibits osteoporosis on ovariectomized rats or postmenopausal women.
    Nilestriol
  • HY-18719
    Endoxifen (Z-isomer)
    		Inhibitor 99.19%
    Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer inhibits PKCβ1 kinase activity. Endoxifen Z-isomer attenuates PKCβ1-activated AKTSer473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer exhibits anticancer activity against hormone-resistant metastatic breast cancer.
    Endoxifen (Z-isomer)
  • HY-132205
    DS45500853
    		Agonist 99.18%
    DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
    DS45500853
  • HY-N6714
    Alternariol
    		Activator 99.88%
    Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol
  • HY-N4183
    Licoflavone C
    		Activator 99.83%
    Licoflavone C is a broad-spectrum antiviral inhibitor with estrogen-like properties. Licoflavone C binds to viral endonuclease (CEN) and inhibits the replication of various bunyaviruses including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus in a non-substrate competitive manner. The IC50 values of Licoflavone C against SFTSV CEN and SFTSV CEN are 35.5 μM and 135.8 μM, respectively, and its Kd value against SFTSV CEN is 9.53 μM. After viral entry into cells, Licoflavone C reduces viral loads in mouse tissues in a dose-dependent manner, and exhibits extremely low cytotoxicity and genotoxicity. Licoflavone C induces apoptosis by increasing caspase 3/7 activity, blocks the cell cycle, and alleviates chemotherapy-induced chromosomal damage. Licoflavone C is applicable to the research on severe fever with thrombocytopenia syndrome and related viral infection mechanisms.
    Licoflavone C
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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