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-135590
    Raloxifene 4-Monomethyl Ether
    Modulator
    Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6.
    Raloxifene 4-Monomethyl Ether
  • HY-N6710R
    α-Zearalenol (Standard)
    Inhibitor
    α-Zearalenol (Standard) is the analytical standard of α-Zearalenol. This product is intended for research and analytical applications. α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.
    α-Zearalenol (Standard)
  • HY-106551
    Mepitiostane
    Mepitiostane is an orally active steroidal antiestrogen. Mepitiostane can be used for the research of breast cancer.
    Mepitiostane
  • HY-B0412S4
    Estriol-d3-1
    Antagonist
    Estriol-d3-1 is the deuterium labeled Estriol.
    Estriol-d<sub>3</sub>-1
  • HY-123047R
    Tibolone (Standard)
    Agonist
    Tibolone (Standard) is the analytical standard of Tibolone. This product is intended for research and analytical applications. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone (Standard)
  • HY-106839
    NKS-01
    Modulator
    NKS-01 is a selective estrogen receptor modulator. NKS-01 can be used for the research of cancer, such as estrogen receptor-positive breast cancer.
    NKS-01
  • HY-149833
    ERRγ inverse agonist 2
    Agonist
    ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities.
    ERRγ inverse agonist 2
  • HY-169367
    ERD-1233
    Degrader
    ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER+ breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)).
    ERD-1233
  • HY-168099
    ERα degrader 10
    Degrader
    ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer.
    ERα degrader 10
  • HY-16470
    SR 16234
    Modulator
    SR 16234 (TAS-108) is a selective estrogen receptor modulator. SR 16234 is promising for research of pain symptoms associated with endometriosis.
    SR 16234
  • HY-181171
    HIT-2
    Inhibitor
    HIT-2 is an estrogen receptor alpha (ERα) inhibitor that can bind to the ERα ligand binding domain. HIT-2 forms stable interactions including hydrogen bonds, π-π stacking, and hydrophobic contacts to disrupt ERα-driven signaling. HIT-2 exhibits antineoplastic activity against breast cancer. HIT-2 can be used for the research of breast cancer.
    HIT-2
  • HY-W020788
    Benoxacor
    Activator 99.39%
    Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.
    Benoxacor
  • HY-169777
    WAY-214156
    Agonist
    WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of ERβ.
    WAY-214156
  • HY-149081
    ERα degrader 6
    Inhibitor
    ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research.
    ERα degrader 6
  • HY-B0141S5
    Estradiol-13C2
    Agonist 98.72%
    Estradiol-13C2 is the 13C-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-<sup>13</sup>C<sub>2</sub>
  • HY-175448
    GNE-1567
    Degrader
    GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a Kd value of 0.03 μM. GNE-1567 is indicated for breast cancer research. (Pink: ligand for target protein (HY-18719); Black: linker; Blue: ligand for E3 ligase (HY-175449)).
    GNE-1567
  • HY-107043
    7β-Hydroxy-epi-androsterone
    Modulator
    7β-Hydroxy-epi-androsterone (7β-Hydroxy-EpiA) can bind to ERβ and has anti-inflammatory and neuroprotective properties. 7β-Hydroxy-epi-androsterone is an endogenous androgenic derivative of dehydroepiandrosterone.
    7β-Hydroxy-epi-androsterone
  • HY-B0234S3
    Estrone-13C2
    Agonist
    Estrone-13C2 is the 13C-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-<sup>13</sup>C<sub>2</sub>
  • HY-135595
    6-Raloxifene-β-D-glucopyranoside
    Antagonist
    6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
    6-Raloxifene-β-D-glucopyranoside
  • HY-163712S
    17-Epiestriol-d5-1
    17-Epiestriol-d5-1 is the deuterium labeled 17-Epiestriol (HY-163712). 17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase.
    17-Epiestriol-d<sub>5</sub>-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.