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-B1403
    Dienestrol
    Agonist 98.08%
    Dienestrol is an orally active nonsteroidal estrogen. Dienestrol prevents the formation of implantation swellings in the uterus by inhibiting ovum discharge.
    Dienestrol
  • HY-118065
    Fenhexamid
    Agonist 99.60%
    Fenhexamid, a botryticide, is a sterol biosynthesis inhibitor. Fenhexamid shows fungicide efficient against the plant pathogenic fungus Botryotinia fuckeliana (Botrytis cinerea).
    Fenhexamid
  • HY-164764
    ADX61623
    Inhibitor 98.84%
    ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease.
    ADX61623
  • 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
  • HY-N0322S2
    Cholesterol-d6-1
    Agonist 99.82%
    Cholesterol-d6-1 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>-1
  • 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-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-B0412R
    Estriol (Standard)
    Antagonist
    Estriol (Standard) is the analytical standard of Estriol. This product is intended for research and analytical applications.
    Estriol (Standard)
  • HY-B0652
    Etonogestrel
    Agonist 99.91%
    Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel
  • HY-W100026
    Galaxolide
    Galaxolide is a polycyclic musk synthetic fragrance. Galaxolide possesses endocrine-disrupting activity and can exert anti-androgenic/estrogenic effects. Galaxolide exhibits in vivo androgenic activity in immature rats. Galaxolide can be used in studies related to endocrine disruption.
    Galaxolide
  • 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-113293BS1
    Estrone sulfate-d4 sodium
    99.39%
    Estrone sulfate-d4 sodium is the deuterium labeled Estrone sulfate sodium (HY-113293B). Estrone sulfate sodium is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate sodium is also a substrate of the OATP1B3 transporter. Estrone sulfate sodium can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate sodium stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate sodium is applicable to breast cancer-related research.
    Estrone sulfate-d<sub>4</sub> sodium
  • HY-B0234S2
    Estrone-d4
    Agonist 99.55%
    Estrone-d4 is the deuterium 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-d<sub>4</sub>
  • HY-14598S
    Diethylstilbestrol-d8
    Agonist 99.74%
    Diethylstilbestrol-d8 is the deuterium labeled Diethylstilbestrol. Diethylstilbestrol, a synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders.
    Diethylstilbestrol-d<sub>8</sub>
  • HY-13738AR
    Raloxifene hydrochloride (Standard)
    Antagonist
    Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
    Raloxifene hydrochloride (Standard)
  • HY-123047
    Tibolone
    Agonist 99.9%
    Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone
  • 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-112100
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1
    Inhibitor 99.18%
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. MC-Val-Cit-PAB-PROTAC ERα Degrader-1 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1
  • HY-145341
    GNE-149
    Antagonist 99.18%
    GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
    GNE-149
  • HY-145716
    Nafoxidine
    Antagonist 98.75%
    Nafoxidine, a nonsteroidal estrogen antagonist, is shown to possess antitumor activity against breast cancer.
    Nafoxidine
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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