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-131586
    3,7-Dihydroxyflavone
    		Modulator 98.04%
    3,7-Dihydroxyflavone (Resogalangin) is a flavonoid phytoestrogen, which can be isolated from Adenophora species. 3,7-Dihydroxyflavone is a modulator of estrogen receptors and an inhibitor of human progesterone metabolizing enzyme AKR1C1 and fungal 17β-hydroxysteroid dehydrogenase and a redox inhibitor (IC50=0.6 and 6.0 μM, respectively). 3,7-Dihydroxyflavone is a fluorescent binding substrate for human serum albumin (HSA) with excitation wavelengths of 370 nm (pH 7.4) and 350 nm (pH 3.5), respectively, and emission wavelength of 515 nm.
    3,7-Dihydroxyflavone
  • HY-103455
    ZK164015
    		99.94%
    ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
    ZK164015
  • HY-W766497
    Alpha-Zearalenol-d7
    Alpha-Zearalenol-d7 is the deuterium labeled α-Zearalenol (HY-N6710). 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.
    Alpha-Zearalenol-d<sub>7</sub>
  • HY-N0791R
    Tectoridin (Standard)
    Tectoridin (Standard) is the analytical standard of Tectoridin. This product is intended for research and analytical applications. Tectoridin is a isoflavone isolated from Maackia amurensis. Tectoridin is a phytoestrogen and activates estrogen and thyroid hormone receptors. Tectoridin exerts the estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway.
    Tectoridin (Standard)
  • HY-149584
    CIDD-0149897
    		Agonist 99.91%
    CIDD-0149897 is a potent, selective and brain-penetrant ERβ agonist. CIDD-0149897 exert antitumor functions in glioblastoma.
    CIDD-0149897
  • HY-153895
    SLU-PP-1072
    		Inhibitor 98.24%
    SLU-PP-1072 is a dual ERRα/γ inverse agonist, used in Prostate cancer (PCa) research. SLU-PP-1072 disrupts PCa cell metabolism, and induces apoptosis via dysregulating cell cycle.
    SLU-PP-1072
  • HY-117153
    GW7604
    		Antagonist 98.0%
    GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist.
    GW7604
  • HY-163561
    CARM1-IN-6
    		Inhibitor 99.59%
    CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC50 of 12.3 μM and a Kd of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer.
    CARM1-IN-6
  • HY-19822D
    Elacestrant (S enantiomer)
    		Inhibitor
    Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
    Elacestrant (S enantiomer)
  • HY-179433
    PROTAC AR Degrader-12
    		Inhibitor
    PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer.
    PROTAC AR Degrader-12
  • HY-13757AS1
    Tamoxifen-d3
    Tamoxifen-d3 is the deuterium labeled Tamoxifen. 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-d<sub>3</sub>
  • HY-18719ES
    Endoxifen-d5
    Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
    Endoxifen-d<sub>5</sub>
  • HY-N2335R
    Coumestrol (Standard)
    		Inhibitor
    Coumestrol (Standard) is the analytical standard of Coumestrol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0377R
    Liquiritigenin (Standard)
    		Agonist
    Tribenoside (Standard) is the analytical standard of Tribenoside. This product is intended for research and analytical applications. Tribenoside is a vasoprotective agent, can be used for the research of hemorrhoids. Tribenoside has mild anti-inflammatory, analgesic, and wound healing properties.
    Liquiritigenin (Standard)
  • HY-79315
    6-Dehydronandrolone acetate
    		Antagonist 99.94%
    6-Dehydronandrolone acetate is a starting material for synthesis of Fulvestrant. Fulvestrant is an estrogen receptor antagonist that can be used for the research of breast cancer.
    6-Dehydronandrolone acetate
  • HY-103451
    (R,R)-THC
    		Antagonist 99.0%
    (R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6.
    (R,R)-THC
  • HY-19822B
    Elacestrant S enantiomer dihydrochloride
    		Inhibitor
    Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
    Elacestrant S enantiomer dihydrochloride
  • HY-143226
    DK1
    		Modulator 99.69%
    DK1 is a potent modulator of estrogen related receptor. DK1 has an ability in reducing blood glucose, and impacts the activity of ERRα receptor. DK1 has the potential for the research of diabetes.
    DK1
  • HY-103451A
    rel-(R,R)-THC
    		Antagonist
    rel-(R,R)-THC is the relative configuration of (R,R)-THC (HY-103451). (R,R)-THC is an ERα agonist and an ERβ antagonist, with Kis of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6.
    rel-(R,R)-THC
  • HY-116896
    LY117018
    		Modulator 99.47%
    LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
    LY117018
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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