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-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one
    		99.37%
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor proagent of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
    10β,17β-dihydroxyestra-1,4-dien-3-one
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride
    		Antagonist 99.63%
    N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
    N-Desmethyltamoxifen hydrochloride
  • HY-18295
    Erteberel
    		Agonist 99.88%
    Erteberel (LY500307) 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.
    Erteberel
  • HY-136242
    UT-34
    		Degrader 98.09%
    UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
    UT-34
  • HY-13556A
    Arzoxifene hydrochloride
    		Modulator 98.00%
    Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
    Arzoxifene hydrochloride
  • HY-B0390
    Mestranol
    		Agonist 99.69%
    Mestranol is an inactive proagent and becomes biologically active on conversion to ethinyl estradiol (EE). Mestranol acts as an estrogen receptor agonist. Mestranol combines with a progestin in vivo and can be used for the research of menopausal hormone or menstrual disorders. Mestranol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mestranol
  • HY-111486
    LSZ-102
    		Degrader 99.94%
    LSZ-102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with an IC50 value of 0.2 nM.
    LSZ-102
  • HY-108414
    (R)-Equol
    		Agonist 98.68%
    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
    (R)-Equol
  • HY-144070
    ErSO-DFP
    		99.56%
    ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO (HY-132247). ErSO-DFP displays antitumor activity against MCF-7 in mice. ErSO-DFP can cross the blood brain barrier.
    ErSO-DFP
  • HY-B0216S
    Ethynyl Estradiol-d4
    		Agonist 99.00%
    Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Ethynyl Estradiol-d<sub>4</sub>
  • HY-B1662
    Hexestrol
    		Agonist 99.79%
    Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.
    Hexestrol
  • HY-N6710
    α-Zearalenol
    		Inhibitor 99.73%
    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.
    α-Zearalenol
  • HY-16950B
    (E)-4-Hydroxytamoxifen
    		Modulator 98.27%
    (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
    (E)-4-Hydroxytamoxifen
  • HY-N6625
    Chlorothalonil
    		Activator 98.15%
    Chlorothalonil is a broad-spectrum foliar fungicide with oral activity. Chlorothalonil can be used to combat fungal diseases in vegetable and crop leaves. Chlorothalonil can alter the microbial community in the soil. Chlorothalonil inhibits spermatogenesis. Chlorothalonil can cause intestinal epithelial barrier dysfunction and fetal toxicity.
    Chlorothalonil
  • HY-N7781
    (-)-(E)-Guggulsterone
    		Agonist 99.19%
    (-)-(E)-Guggulsterone ((E)-Guggulsterone) is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
    (-)-(E)-Guggulsterone
  • HY-150210
    FSHR agonist 1
    		Agonist 99.45%
    FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR.
    FSHR agonist 1
  • HY-107245
    Segetalin B
    		Ligand 99.56%
    Segetalin B, an orally active cyclopentapeptide found in Vaccaria segetalis, possesses estrogen-like activity. Segetalin B promotes mineralization of ovariectomized rat-derived bone marrow mesenchymal stem cells (BMSCs) in vitro and increases the level of osteocalcin, BMP-2, ALP, and SIRT1 activity. Segetalin B is promising for research of post-menopausal osteoporosis (PMOP).
    Segetalin B
  • HY-143227
    DK3
    		Agonist 99.82%
    DK3 is a potent and selective estrogen-related receptor alpha (ERRα) agonist.
    DK3
  • HY-A0036D
    Bazedoxifene acetate-D
    		99.88%
    Bazedoxifene (acetate)-D (TSE-424 (acetate)-D) is the D-crystal form compound of Bazedoxifene acetate (HY-A0036). Bazedoxifene acetate is an orally active, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively.
    Bazedoxifene acetate-D
  • HY-B1403
    Dienestrol
    		Agonist 98.08%
    Dienestrol is an orally active nonsteroidal estrogen. Dienestrol prevents the formation of implantation swellings in the uterus by inhibiting ovum discharge.
    Dienestrol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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