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. 상품명 효과 Purity Chemical Structure
  • HY-N15700
    Toralactone 9-O-triglucoside
    Toralactone 9-O-triglucoside (Compound 2) is a phenolic trisaccharide. Toralactone 9-O-triglucoside can be isolated from Cassia seed. Toralactone 9-O-triglucoside can be used in the research of estrogen-related diseases such as breast cancer, prostate cancer, osteoporosis and cardiovascular disease.
    Toralactone 9-O-triglucoside
  • HY-143253
    Estrogen receptor antagonist 7
    Antagonist
    Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities.
    Estrogen receptor antagonist 7
  • HY-149969
    ER degrader 4
    Degrader
    ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity.
    ER degrader 4
  • HY-174870
    PROTAC ERα Degrader-11
    Degrader
    PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)).
    PROTAC ERα Degrader-11
  • HY-135596
    Raloxifene dimethyl ester hydrochloride
    Control
    Raloxifene dimethyl ester hydrochloride is an analog of Raloxifene, extracted from patent US5464845A, compound 28.
    Raloxifene dimethyl ester hydrochloride
  • HY-13738S3
    Raloxifene-d10
    Modulator
    Raloxifene-d10 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
    Raloxifene-d<sub>10</sub>
  • HY-168869
    Tamoxifen-PEG-Clozapine
    Degrader
    Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer. (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))
    Tamoxifen-PEG-Clozapine
  • HY-122359A
    rel-Levormeloxifene
    Modulator
    rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells.
    rel-Levormeloxifene
  • HY-B1630
    Stilbestrol dipropionate
    Stilbestrol dipropionate is an estrogen-like compound with hormone suppressive activity for recurrent prostate cancer. Stilbestrol dipropionate can be used to suppress diseases associated with estrogen deficiency.
    Stilbestrol dipropionate
  • HY-168270
    PROTAC ER Degrader-11
    Degrader
    PROTAC ER Degrader-11 (Example 26-1) is a potent PROTAC ER degrader, with the IC50 of 0.66 nM. PROTAC ER Degrader-11 plays an important role in cancer research(Sturcture Note:(Blue: Cereblon ligand (HY-W797329), Black: linker (HY-W262798);Pink: ER ligand (HY-168271)).
    PROTAC ER Degrader-11
  • HY-W100026S
    Galaxolide-d6 (mixture of diastereomers) (>80%)
    Galaxolide-d6 (mixture of diastereomers) (>80%) is the deuterium labeled Galaxolide (HY-W100026). Galaxolide can induce estrogenic activity (Estrogen Receptor/ERR), trigger oxidative stress and genotoxicity, and induce EROD and GST (Glutathione S-transferase) enzyme activity.
    Galaxolide-d<sub>6</sub> (mixture of diastereomers) (>80%)
  • HY-155492
    ERα degrader 7
    Degrader
    ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research.
    ERα degrader 7
  • HY-180306
    Fluoroestradiol
    Ligand
    Fluoroestradiol is an Estrogen receptor PET imaging tracer precursor. Fluoroestradiol, when radiolabeled with 18F, can be used as an Estrogen receptor PET imaging tracer. 18F-Fluoroestradiol exhibits the highest uptake selectivity and target-to-background ratio among
    several 18F-labeled estrogens. 18F-Fluoroestradiol has demonstrated Estrogen receptor expression in normal brain tissues and in meningiomas. 18F-Fluoroestradiol can quantify regional Estrogen receptor expression in breast cancer. 18F-Fluoroestradiol has potential applications in assessing and monitoring heterogeneity in ovarian cancer.
    Fluoroestradiol
  • HY-15731S1
    Estetrol-d4 (Major)
    Estetrol-d4 (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research.
    Estetrol-d<sub>4</sub> (Major)
  • HY-122411
    Panomifene
    Inhibitor
    Panomifene (EGIS 5650) is a tamoxifen (HY-13757A) analog with an antiestrogenic activity. Panomifene can be used in the research of breast cancer.
    Panomifene
  • HY-N2026S
    Propylparaben-d7
    Agonist
    Propylparaben-d7 (Propyl parahydroxybenzoate-d7) is the deuterium labeled Propylparaben (HY-N2026). Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is an orally active weak estrogen receptor agonist. Propylparaben regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
    Propylparaben-d<sub>7</sub>
  • HY-113293
    Estrone sulfate
    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
  • HY-103453
    (R)-DPN
    Chemical
    (R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively.
    (R)-DPN
  • HY-103452
    RU58668
    Antagonist
    RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research.
    RU58668
  • HY-N6714R
    Alternariol (Standard)
    Activator
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. 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 (Standard)
Cat. No. 상품명 / Synonyms Species Source
Cat. No. 상품명 / Synonyms Application Reactivity

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