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-145848
    ERRγ agonist-1
    Agonist 98.02%
    ERRγ agonist-1 is a potent ERRγ agonist. ERRγ agonist-1 increases transcriptional activities of ERRγ. ERRγ agonist-1 has the potential for the research of neuropsychological disorders.
    ERRγ agonist-1
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one
    99.12%
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor proagent of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
    10β,17β-dihydroxyestra-1,4-dien-3-one
  • HY-B0708
    β-Estradiol 17-acetate
    Agonist 99.93%
    β-Estradiol 17-acetate is a metabolite of estradiol.
    β-Estradiol 17-acetate
  • HY-143201
    DS20362725
    Agonist 99.34%
    DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 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 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
    DS20362725
  • HY-107245
    Segetalin B
    Ligand 99.51%
    Segetalin B, an orally active cyclopentapeptide found in Vaccaria segetalis, possesses estrogen-like activity. Segetalin B promotes mineralization of ovariectomized rat-derived bone marrow mesenchymal stem cells (BMSCs) in vitro and increases the level of osteocalcin, BMP-2, ALP, and SIRT1 activity. Segetalin B is promising for research of post-menopausal osteoporosis (PMOP).
    Segetalin B
  • HY-101271
    WAY-200070
    Agonist 99.57%
    WAY-200070 is a selective estrogen receptor β (ERβ) agonist with an IC50 of 2.3 nM.
    WAY-200070
  • HY-U00425
    PROTAC ERRα ligand 1
    Antagonist 99.47%
    PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively.
    PROTAC ERRα ligand 1
  • HY-119437
    FLTX1
    Inhibitor 99.75%
    FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.
    FLTX1
  • 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-150210
    FSHR agonist 1
    Agonist 99.45%
    FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR.
    FSHR agonist 1
  • HY-159957
    BAY-184
    Inhibitor 99.00%
    BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth.
    BAY-184
  • HY-143227
    DK3
    Agonist 99.82%
    DK3 is a potent and selective estrogen-related receptor alpha (ERRα) agonist.
    DK3
  • HY-N3755
    Dihydroresveratrol
    Modulator 99.41%
    Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
    Dihydroresveratrol
  • HY-121528
    Nilestriol
    98.93%
    Nilestriol is a estriol derivative, which inhibits osteoporosis on ovariectomized rats or postmenopausal women.
    Nilestriol
  • HY-B0672R
    Estradiol valerate (Standard)
    Agonist
    Estradiol valerianate (Standard) is the analytical standard of Estradiol valerianate. This product is intended for research and analytical applications. Estradiol valerate (β-Estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
    Estradiol valerate (Standard)
  • HY-13556A
    Arzoxifene hydrochloride
    Modulator 98.00%
    Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
    Arzoxifene hydrochloride
  • HY-B1662
    Hexestrol
    Agonist 99.89%
    Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.
    Hexestrol
  • HY-41570
    3-Formylsalicylic acid
    Inhibitor 98.46%
    3-Formylsalicylic acid is a noncompetitive estrone sulfatase inhibitor with an IC50 value of 0.15 mM, a Ki value of 0.12 mM. 3-Formylsalicylic acid shows a low acute toxicity.
    3-Formylsalicylic acid
  • HY-A0036D
    Bazedoxifene (acetate)-D
    99.93%
    Bazedoxifene (acetate)-D (TSE-424 (acetate)-D) is the D-crystal form compound of Bazedoxifene acetate (HY-A0036). Bazedoxifene acetate is an orally active, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively.
    Bazedoxifene (acetate)-D
  • HY-139185
    PROTAC ERRα Degrader-3
    Inhibitor 98.82%
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
    PROTAC ERRα Degrader-3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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