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-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one
    98.89%
    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-119437
    FLTX1
    Inhibitor 99.75%
    FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.
    FLTX1
  • HY-121528
    Nilestriol
    98.93%
    Nilestriol is a estriol derivative, which inhibits osteoporosis on ovariectomized rats or postmenopausal women.
    Nilestriol
  • HY-U00425
    PROTAC ERRα ligand 1
    Antagonist 99.47%
    PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively.
    PROTAC ERRα ligand 1
  • HY-U00178
    Idoxifene
    Modulator 99.43%
    Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
    Idoxifene
  • HY-111484
    GDC-0927
    Antagonist 99.98%
    GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
    GDC-0927
  • HY-12825
    BHPI
    Inhibitor ≥98.0%
    BHPI is a nuclear receptor ERα inhibitor. BHPI activates PLCγ and UPR. BHPI has antitumor activity against breast, endometrial, and ovarian cancers.
    BHPI
  • HY-B0672R
    Estradiol valerate (Standard)
    Agonist 99.87%
    Estradiol valerianate (Standard) is the analytical standard of Estradiol valerianate. This product is intended for research and analytical applications. Estradiol valerate (β-Estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
    Estradiol valerate (Standard)
  • HY-B1662
    Hexestrol
    Agonist 99.89%
    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-41570
    3-Formylsalicylic acid
    Inhibitor 98.06%
    3-Formylsalicylic acid is a noncompetitive estrone sulfatase inhibitor with an IC50 value of 0.15 mM, a Ki value of 0.12 mM. 3-Formylsalicylic acid shows a low acute toxicity.
    3-Formylsalicylic acid
  • HY-A0036D
    Bazedoxifene (acetate)-D
    99.93%
    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-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-B0390
    Mestranol
    Agonist 99.97%
    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-139185
    PROTAC ERRα Degrader-3
    Inhibitor 98.82%
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
    PROTAC ERRα Degrader-3
  • HY-112611
    H3B-5942
    Inhibitor 99.73%
    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations.
    H3B-5942
  • HY-137449
    Rintodestrant
    Antagonist 99.91%
    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.
    Rintodestrant
  • HY-B0141S
    Estradiol-d3
    Agonist 98.60%
    Estradiol-d3 is the 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>3</sub>
  • 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-159957
    BAY-184
    Inhibitor 99.00%
    BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth.
    BAY-184
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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