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-W653896
    Alternariol-d2
    Activator
    Alternariol-d2 is deuterium labeled Alternariol. 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-d<sub>2</sub>
  • HY-168644
    Erα-IN-1
    Inhibitor
    Erα-IN-1 (compound 3c) is an inhibitor of estrogen receptor α (ERα), blocking ERa activity in MCF7/ERE-LUC cells..
    Erα-IN-1
  • HY-118861S1
    Enclomiphene-d4
    Inhibitor 99.85%
    Enclomiphene-d4 ((E)-Clomiphene-d4) is a deuterium labeled Enclomiphene. Enclomiphen?is a potent and orally active?estrogen receptor?antagonist with antioestrogenic property.
    Enclomiphene-d<sub>4</sub>
  • HY-164463
    BMI-135
    Agonist
    BMI-135 is a selective estrogen mimic, that exhibits agonist activity for estrogen receptor. BMI-135 induces rapid endoplasmic reticulum stress response (UPR) and apoptosis in breast cancer cells.
    BMI-135
  • HY-W1005067
    EN171
    Antagonist
    EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol.
    EN171
  • HY-30270R
    Mequinol (Standard)
    Activator
    Mequinol (Standard) is the analytical standard of Mequinol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0390R
    Mestranol (Standard)
    Agonist
    Mestranol (Standard) is the analytical standard of Mestranol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-118065R
    Fenhexamid (Standard)
    Agonist
    Fenhexamid (Standard) is the analytical standard of Fenhexamid. This product is intended for research and analytical applications. Fenhexamid, a botryticide, is a sterol biosynthesis inhibitor. Fenhexamid shows fungicide efficient against the plant pathogenic fungus Botryotinia fuckeliana (Botrytis cinerea).
    Fenhexamid (Standard)
  • HY-135583
    LY88074 Trimethyl ether
    LY88074 Trimethyl ether (Example 1) is useful for the inhibition of the various estrogen deficient conditions, which are associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia.
    LY88074 Trimethyl ether
  • HY-B1403R
    Dienestrol (Standard)
    Agonist
    Dienestrol (Standard) is the analytical standard of Dienestrol. This product is intended for research and analytical applications.
    Dienestrol (Standard)
  • HY-B0723S2
    Ospemifene-d5
    Modulator
    Ospemifene-d5 (FC-1271a-d5) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
    Ospemifene-d<sub>5</sub>
  • HY-N6678R
    Zearalanone (Standard)
    Activator
    Zearalanone (Standard) is the analytical standard of Zearalanone. This product is intended for research and analytical applications. Zearalenone is a nonsteroidal estrogenic mycotoxin produced by Fusarium species, which colonizes several grains. Zearalenone has low acute toxicity and carcinogenicity. Due to its agonistic effect on the estrogen receptor, Zearalenone exhibits distinct estrogenic and anabolic properties in several animal species, resulting in severe effects on the reproductive system.
    Zearalanone (Standard)
  • HY-B1176R
    Equilin (Standard)
    Agonist
    Equilin (Standard) is the analytical standard of Equilin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-124414AR
    4'-Hydroxytamoxifen TFA (Standard)
    4'-Hydroxytamoxifen (TFA) (Standard) is the analytical standard of 4'-Hydroxytamoxifen (TFA). This product is intended for research and analytical applications. 4'-Hydroxytamoxifen TFA is a salt form of a metabolite of Tamoxifen. 4'-Hydroxytamoxifen TFA has a higher affinity for ER than Tamoxifen. 4'-Hydroxytamoxifen TFA induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells[1].
    4'-Hydroxytamoxifen TFA (Standard)
  • HY-B1662R
    Hexestrol (Standard)
    Agonist
    Hexestrol (Standard) is the analytical standard of Hexestrol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-U00216
    NNC45-0781
    Agonist
    NNC45-0781 is a tissue-selective estrogen partial-agonist.
    NNC45-0781
  • HY-U00323
    Carbazole derivative 1
    Inhibitor
    Carbazole derivative 1 is a carbazole derivative which can be used to reduce androgen or oestrogen levels in mammals, including humans.
    Carbazole derivative 1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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