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-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-101447A
    SI-2 hydrochloride
    		Inhibitor 98.06%
    SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.
    SI-2 hydrochloride
  • HY-B0141S2
    Estradiol-d5
    		Agonist 99.73%
    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-113960
    ERRα antagonist-1
    		Antagonist 99.71%
    ERRα antagonist-1 (Compound A) is a selective and high affinity agonist for estrogen-related receptor α (ERRα). ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively.
    ERRα antagonist-1
  • 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-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-B0234R
    Estrone (Standard)
    		Agonist
    Estrone (Standard) is the analytical standard of Estrone. This product is intended for research and analytical applications. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.
    Estrone (Standard)
  • HY-33353
    GSK-4716
    		Agonist 99.63%
    GSK-4716 is a selective ERRβ/γ agonist.
    GSK-4716
  • HY-15731
    Estetrol
    		Modulator 99.76%
    Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research.
    Estetrol
  • HY-13636R
    Fulvestrant (Standard)
    		Antagonist
    Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
    Fulvestrant (Standard)
  • HY-118861A
    Enclomiphene citrate
    		Antagonist 99.93%
    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-P3343A
    hFSH-β-(33-53) TFA
    		Agonist 99.56%
    hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells.
    hFSH-β-(33-53) TFA
  • HY-101405
    Gestrinone
    		Inhibitor 99.76%
    Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM. Gestrinone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Gestrinone
  • HY-145572A
    Imlunestrant tosylate
    		Degrader 99.86%
    Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).
    Imlunestrant tosylate
  • HY-N0553
    Gypenoside XVII
    		Activator 99.69%
    Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
    Gypenoside XVII
  • HY-N3755
    Dihydroresveratrol
    		Modulator 99.69%
    Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
    Dihydroresveratrol
  • HY-12864
    Brilanestrant
    		Inhibitor 99.85%
    Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
    Brilanestrant
  • HY-156197
    Biotin-cholesterol
    		Agonist
    Biotin-cholesterol is a biotinylated form of Cholesterol (HY-N0322). Biotin-cholesterol can be used in the synthesis of biotin-conjugated liposomes and micelles for drug delivery.
    Biotin-cholesterol
  • 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
  • HY-B1176
    Equilin
    		Agonist 99.91%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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