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-113293B
    Estrone sulfate sodium
    		99.84%
    Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). Estrone sulfate can be used for the research of breast cancer.
    Estrone sulfate sodium
  • HY-B0216
    Ethinylestradiol
    		Agonist 99.91%
    Ethinylestradiol is an orally active steroidal estrogen. Ethinylestradiol is widely used in research on menopausal symptoms, gynecological conditions, and certain hormone-sensitive cancers.
    Ethinylestradiol
  • HY-B0412
    Estriol
    		Modulator 99.68%
    Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects.
    Estriol
  • HY-14598
    Diethylstilbestrol
    		Agonist 99.62%
    Diethylstilbestrol is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor..
    Diethylstilbestrol
  • HY-13738
    Raloxifene
    		Modulator 99.62%
    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
  • HY-N2335
    Coumestrol
    		Inhibitor 98.28%
    Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC50 of 50 μM.
    Coumestrol
  • HY-13757AR
    Tamoxifen (Standard)
    		Modulator 99.76%
    Tamoxifen (Standard) is the analytical standard of Tamoxifen. This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen (Standard)
  • HY-100583
    (-)-(S)-Equol
    		99.68%
    (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
    (-)-(S)-Equol
  • HY-103450
    G36
    		Antagonist 99.66%
    G-36 is a cell permeable non-steroidal antagonist of G-protein-coupled estrogen receptor (GPER/GPR30) which selectively inhibits estrogen-mediated activation of PI3K by GPER, but not by ERα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM).
    G36
  • HY-B0672
    Estradiol valerate
    		Agonist 99.76%
    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
  • HY-128600
    ERD-308
    		Inhibitor 99.17%
    ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).
    ERD-308
  • HY-15449
    Kaempferide
    		Inhibitor 99.35%
    Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.
    Kaempferide
  • HY-N0835
    (20S)-Protopanaxatriol
    		Agonist 99.91%
    (20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
    (20S)-Protopanaxatriol
  • HY-B1100
    Estradiol cypionate
    		Inhibitor 99.67%
    Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.
    Estradiol cypionate
  • HY-B1176
    Equilin
    		Agonist 99.91%
    Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism.
    Equilin
  • HY-133017
    Amcenestrant
    		Antagonist 99.59%
    SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer.
    Amcenestrant
  • HY-12864
    Brilanestrant
    		Inhibitor 99.95%
    Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
    Brilanestrant
  • HY-N0233
    Bavachin
    		Agonist 99.94%
    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
  • HY-103454
    MPP dihydrochloride
    		Modulator 99.06%
    MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
    MPP dihydrochloride
  • HY-A0038
    Lasofoxifene tartrate
    		Modulator 99.92%
    Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis.
    Lasofoxifene tartrate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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