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-W150752
    Triphenylethylene
    Antagonist
    Triphenylethylene is an aromatic hydrocarbon that possesses weak estrogenic activity. Triphenylethylene antiestrogens relax duodenal intestinal muscle via a mechanism that involves inhibition of L-type Ca2+ channels but not activation of K+ channels.
    Triphenylethylene
  • HY-B1176S1
    Equilin-d2
    Agonist
    Equilin-d2 (7-Dehydroestrone-d2) is deuterium labeled Equilin. 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-d<sub>2</sub>
  • HY-13738R
    Raloxifene (Standard)
    Modulator
    Raloxifene (Standard) is the analytical standard of Raloxifene. This product is intended for research and analytical applications. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
    Raloxifene (Standard)
  • HY-B1617AS2
    Zuclomiphene d10 Citrate salt
    Modulator
    Zuclomiphene d10 Citrate salt is deuterium labeled Zuclomiphene (citrate). Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.
    Zuclomiphene d<sub>10</sub> Citrate salt
  • HY-B0316S1
    Avobenzone-d3
    Antagonist
    Avobenzone-d3 is deuterium labeled Avobenzone. 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-d<sub>3</sub>
  • HY-N4069
    Lupinalbin A
    Agonist
    Lupinalbin A (Boeravinone L) is a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor with IC50 values ​​of 45.2 and 53.4 µM, respectively. Lupinalbin A exhibits antidiabetic activity.
    Lupinalbin A
  • HY-169916
    GuaB-IN-1
    Inhibitor
    GuaB-IN-1 (Compound 15) exhibits high potency against M.tb with a MIC value of 0.25 μM. GuaB-IN-1 has a favorable 28% hERG inhibition profile at 10 μM. GuaB-IN-1 is promising for research of tuberculosis.
    GuaB-IN-1
  • HY-124114
    4-Hydroxytoremifene
    4-Hydroxytoremifene (4-OH-TOR) is an estrogen receptor antagonist that blocks the uterus's ability to absorb estradiol.
    4-Hydroxytoremifene
  • 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
    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-124414A
    4'-Hydroxytamoxifen TFA
    99.43%
    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.
    4'-Hydroxytamoxifen TFA
  • 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-B1234R
    Octinoxate (Standard)
    Modulator
    Octinoxate (Standard) is the analytical standard of Octinoxate. This product is intended for research and analytical applications. Octinoxate (Octyl methoxycinnamate) is an organic compound that is an ingredient in some sunscreens and lip balms, primarily used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage and can be used to reduce the appearance of scars. Octinoxate also has a complex androgenic and estrogenic effect.
    Octinoxate (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-A0087R
    Octocrylene (Standard)
    Activator
    Octocrylene (Standard) is the analytical standard of Octocrylene. This product is intended for research and analytical applications. Octocrylene is an organic ultraviolet (UV) filter which absorbs mainly UVB radiation and short UVA wavelengths. Octocrylene has the potential for using in various cosmetic products to either provide an appropriate sun protection factor in sunscreen products or to protect cosmetic formulations from UV radiation.
    Octocrylene (Standard)
  • HY-B0463R
    Clomiphene (citrate) (Standard)
    Modulator
    Clomiphene (citrate) (Standard) is the analytical standard of Clomiphene (citrate). This product is intended for research and analytical applications. Clomiphene citrate (Clomifene citrate) is an orally active estrogen-receptor modulator. Clomiphene citrate has anti-cancer actixity, induces perturbations during meiotic maturation and cytogenetic abnormalities and ameliorates in managing psychiatric and cognitive impairment.
    Clomiphene (citrate) (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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