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-N1507R
    Tracheloside (Standard)
    		Inhibitor
    Tracheloside (Standard) is the analytical standard of Tracheloside. This product is intended for research and analytical applications. Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.
    Tracheloside (Standard)
  • HY-106828
    E2-CDS
    E2-CDS (Estradiol 17-Dihydrotrigonelline) is a redox-based chemical delivery system for estradiol (E2). E2-CDS is capable of sustained and brain-selective delivery of estradiol.
    E2-CDS
  • HY-111845
    Estrone-N-O-C1-amido
    Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
    Estrone-N-O-C1-amido
  • HY-W749028
    ERα ligand 4
    		Ligand
    ERα ligand 4 is a ligand of ERα and can be used for the synthesis of PROTACs, such as NEP168 (HY-180959).
    ERα ligand 4
  • HY-B0141S4
    Estradiol-13C6
    		Agonist
    Estradiol-13C6 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>6</sub>
  • HY-16950AR
    (E/Z)-4-Hydroxytamoxifen (Standard)
    		Modulator
    (E/Z)-4-Hydroxytamoxifen (Standard) is the analytical standard of (E/Z)-4-Hydroxytamoxifen. This product is intended for research and analytical applications. (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity.
    (E/Z)-4-Hydroxytamoxifen (Standard)
  • HY-W744064
    Diethylstilbestrol-d4
    Diethylstilbestrol-d4 is the deuterium labeled Diethylstilbestrol (HY-14598). 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-d<sub>4</sub>
  • HY-18295A
    rel-Erteberel
    		Agonist 99.63%
    rel-Erteberel is rel isomer of Erteberel (HY-18295). Erteberel is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities.
    rel-Erteberel
  • HY-B0652R
    Etonogestrel (Standard)
    		Agonist
    Etonogestrel (Standard) is the analytical standard of Etonogestrel. This product is intended for research and analytical applications. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel (Standard)
  • HY-B1830R
    Estradiol enanthate (Standard)
    Estradiol enanthate (Standard) is the analytical standard of Estradiol enanthate. Estradiol enanthate (E2EN) is a shorter-acting estrogen. Estradiol enanthate is an injectable contraceptive in combination with Dihydroxyprogesterone acetophenide. Estradiol enanthate promotes withdrawal bleeding, in a pattern similar to menstruation.
    Estradiol enanthate (Standard)
  • HY-N0377S
    Liquiritigenin-d4
    Liquiritigenin-d4 (4',7-Dihydroxyflavanone-d4) is the deuterium labeled Liquiritigenin (HY-N0377). Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
    Liquiritigenin-d<sub>4</sub>
  • HY-B0652S1
    Etonogestrel-d6
    		Agonist
    Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel-d<sub>6</sub>
  • HY-177011
    ERRγ-IN-1
    		Inhibitor
    ERRγ-IN-1 is a ERRγ inhibitor with an IC50 of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma.
    ERRγ-IN-1
  • HY-155196
    ER degrader 6
    		Degrader
    ER degrader 6 (compound 35s) is a potent Estrogen Receptor (ER)α degrader. ER degrader 6 disrupts the microtubule network by restraining tubulin polymerization. ER degrader 6 suppresses tumor growth without noticeable poisonousness.
    ER degrader 6
  • HY-186074
    ERβ agonist-2
    		Inhibitor
    ERβ agonist-2 (Page 72) is a selective ERβ agonist with an EC50 of 800 nM or lower. ERβ agonist-2 selectively inhibits T cell activation and/or proliferation, thereby reducing circulating T cell levels in subjects, without exerting significant effects on circulating neutrophil, monocyte or B cell levels. ERβ agonist-2 is applicable to studies of chronic heart failure after myocardial infarction, as well as graft-versus-host disease, multiple sclerosis and experimental autoimmune encephalomyelitis.
    ERβ agonist-2
  • HY-B1403S1
    E,E-Dienestrol-d6-1
    		Agonist
    E,E-Dienestrol-d6-1 is a deuterated labeled Dienestrol.
    E,E-Dienestrol-d<sub>6</sub>-1
  • HY-180850
    ERB-2
    		Degrader
    ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.
    ERB-2
  • HY-121198
    Dimestrol
    Dimestrol (Diethylstilbestrol dimethyl ether) is a precursor of Diethylstilbestrol (HY-14598).
    Dimestrol
  • HY-13556
    Arzoxifene
    		Modulator
    Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
    Arzoxifene
  • HY-N3755R
    Dihydroresveratrol (Standard)
    		Modulator
    Clofarabine (Standard) is the analytical standard of Clofarabine. This product is intended for research and analytical applications. Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit.
    Dihydroresveratrol (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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