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-D2280
    Estrogen receptor β/HDAC probe 1
    Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC.
    Estrogen receptor β/HDAC probe 1
  • HY-B1623R
    Cyproterone (Standard)
    Cyproterone (Standard) is the analytical standard of Cyproterone. This product is intended for research and analytical applications. Cyproterone is an antiandrogen that suppresses the actions of testosterone via blocking androgen receptors. Cyproterone’s acetate form can be used in the research of hypersexuality and prostate cancer.
    Cyproterone (Standard)
  • HY-N8075
    Artonin U
    		Ligand
    Artonin U is an artonin. Artonin U can be isolated from Artocarpus species. Artonin U binds to hERα, as measured by docking score and Prime MM-GBSA binding free energy evaluation. Artonin U can be used in breast cancer research.
    Artonin U
  • HY-106056
    Zindoxifene
    		Agonist
    Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer.
    Zindoxifene
  • HY-175445
    GNE-5472
    		Degrader
    GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.
    GNE-5472
  • HY-W142795
    4-sec-Butylphenol
    		Agonist
    4-sec-Butylphenol (4-sec-BP) is an androgen receptor ligand that binds to the androgen receptor with a pIC50 of 4.07. 4-sec-Butylphenol is an estrogen receptor agonist. 4-sec-Butylphenol can be found in industrial effluents, in production water of oil and gas platforms, as well as in river water samples.
    4-sec-Butylphenol
  • HY-19822S2
    Elacestrant-d10
    		Degrader
    Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER+ breast cancer cell lines in vitro and in vivo.
    Elacestrant-d<sub>10</sub>
  • HY-122359B
    Levormeloxifene fumarate
    		Modulator
    Levormeloxifene (fumarate) is a stable salt form of Levormeloxifene. Levormeloxifene (fumarate) is an estrogen receptor modulator that plays an important role in prevention of postmenopausal bone loss.
    Levormeloxifene fumarate
  • HY-N0233R
    Bavachin (Standard)
    		Agonist
    Bavachin (Standard) is the analytical standard of Bavachin. This product is intended for research and analytical applications. Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
    Bavachin (Standard)
  • HY-160563
    PROTAC ERα Degrader-8
    		Degrader
    PROTAC ERα Degrader-8 (compound ii-56) is a potent PROTAC degrader of Erα, with DC50 of 0.000006 μM in MCF7 cells.
    PROTAC ERα Degrader-8
  • HY-176364
    AZD9496-O-C3-O-C3-O-C-acid
    		Inhibitor
    AZD9496-O-C3-O-C3-O-C-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for ERα (HY-12870) and a PROTAC linker, which recruits E3 ligases. AZD9496-O-C3-O-C3-O-C-acid can be used for synthesis of PROTAC AZ'6421 (HY-135312).
    AZD9496-O-C3-O-C3-O-C-acid
  • HY-P11153
    HGH fragment 176-191
    		Ligand
    HGH fragment 176-191 is a fragment of Human Growth Hormone. HGH fragment 176-191 binds with high affinity to Ki-67, MiB protein, and the estrogen receptor. HGH fragment 176-191 enhances the toxicity of Doxorubicin (HY-15142A)-loaded Chitosan nanoparticles against breast cancer.
    HGH fragment 176-191
  • HY-174453
    PROTAC ERα Degrader-12
    		Degrader
    PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)).
    PROTAC ERα Degrader-12
  • HY-143267
    Estrogen receptor antagonist 8
    		Antagonist
    Estrogen receptor antagonist 8 is a potent ER-antagonist with in vivo anti-uterotrophic potential (EC50 = 4.160 μM).
    Estrogen receptor antagonist 8
  • HY-170339
    ER ligand-5
    		Ligand
    ER ligand-5 is the ligand for estrogen receptor, that can be used as ligand for target protein for PROTAC synthesis of PROTAC ERα Degrader-10 (HY-170336).
    ER ligand-5
  • HY-113293S1
    Estrone sulfate-d4 TEA
    Estrone sulfate-d4 TEA is the deuterium labeled Estrone sulfate TEA. Estrone sulfate is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate is also a substrate of the OATP1B3 transporter. Estrone sulfate can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate 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 is applicable to breast cancer-related research.
    Estrone sulfate-d<sub>4</sub> TEA
  • HY-179232
    ERα antagonist 2
    		Antagonist
    ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer.
    ERα antagonist 2
  • HY-B1192S
    Estradiol benzoate-d3
    		Agonist 99.0%
    Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
    Estradiol benzoate-d<sub>3</sub>
  • HY-N2026AR
    Propylparaben sodium (Standard)
    		Agonist
    Propylparaben (Propyl parahydroxybenzoate) sodium (Standard) is the analytical standard of Propylparaben sodium (HY-N2026A). Propylparaben (Propyl parahydroxybenzoate) sodium is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben sodium is an orally active weak estrogen receptor agonist. Propylparaben sodium regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben sodium is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
    Propylparaben sodium (Standard)
  • HY-180851
    ER ligand-14
    		Ligand
    ER ligand-14 is an estrogen receptor (ER) ligand. ER ligand-14 can serve as a ligand for target protein for PROTAC, and can be used to develop and design degradative agents for PROTAC ERβ, such as ERB-2 (HY-180850). ERB-2 displays favorable antiproliferative activity against Osimertinib (HY-15772) resistance NSCLC cells.
    ER ligand-14
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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