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. Product Name Effect Purity Chemical Structure
  • HY-B1234
    Octinoxate
    Modulator 99.84%
    Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate
  • HY-W013935
    Bisphenol B
    Agonist 99.34%
    Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties.
    Bisphenol B
  • HY-118861A
    Enclomiphene citrate
    Antagonist 99.96%
    Enclomiphene ((E)-Clomiphene) citrate is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene citrate can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
    Enclomiphene citrate
  • HY-B0845
    Prochloraz
    Antagonist 99.85%
    Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz
  • HY-112100
    PROTAC ERα Degrader-5
    Inhibitor 98.96%
    PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    PROTAC ERα Degrader-5
  • HY-13724B
    Pipendoxifene hydrochloride
    Modulator 99.83%
    Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer.
    Pipendoxifene hydrochloride
  • HY-13724
    Pipendoxifene
    Modulator 99.93%
    Pipendoxifene is a selective estrogen receptor modulator (SERM).
    Pipendoxifene
  • HY-N0322S5
    Cholesterol-13C2
    Agonist 99.76%
    Cholesterol-13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
    Cholesterol-<sup>13</sup>C<sub>2</sub>
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride
    Antagonist 99.93%
    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-30270
    Mequinol
    Activator 99.98%
    Mequinol (4-Methoxyphenol)yes MercurialisOne of the bioactive ingredients, mainly used for skin discoloration. MequinolIs an antioxidant that has additive/synergistic effects on carcinogenesis when combined with other phenolic antioxidants. Mequinolalso promote hERαDependent chaperone production with potential estrogenic activity.
    Mequinol
  • HY-B0316
    Avobenzone
    Antagonist ≥98.0%
    Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
    Avobenzone
  • HY-18719
    Endoxifen (Z-isomer)
    Inhibitor 99.19%
    Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
    Endoxifen (Z-isomer)
  • 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-14590R
    Kaempferol (Standard)
    Inhibitor
    Kaempferol (Standard) is the analytical standard of Kaempferol. This product is intended for research and analytical applications. Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
    Kaempferol (Standard)
  • HY-N6714
    Alternariol
    Activator 99.88%
    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
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one
    99.12%
    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-B0708
    β-Estradiol 17-acetate
    Agonist 99.93%
    β-Estradiol 17-acetate is a metabolite of estradiol.
    β-Estradiol 17-acetate
  • HY-B0141S2
    Estradiol-d5
    Agonist 99.88%
    Estradiol-d5 is deuterium 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-d<sub>5</sub>
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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