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-112098
    PROTAC ERα Degrader-1
    Inhibitor
    PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
    PROTAC ERα Degrader-1
  • HY-111846
    PROTAC ERα Degrader-2
    Degrader 98.92%
    PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)).
    PROTAC ERα Degrader-2
  • HY-149480
    ERD-3111
    Degrader 98.72%
    ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer.
    ERD-3111
  • HY-112596A
    H3B-6545 hydrochloride
    Antagonist 99.16%
    H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
    H3B-6545 hydrochloride
  • HY-135309
    PROTAC ER Degrader-4
    Inhibitor 98.78%
    PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
    PROTAC ER Degrader-4
  • HY-141551
    GNE-274
    Degrader 98.00%
    GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
    GNE-274
  • HY-150693
    Estrogen receptor β antagonist 2
    Antagonist 98.39%
    Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively.
    Estrogen receptor β antagonist 2
  • HY-N6710
    α-Zearalenol
    Inhibitor 99.63%
    α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.
    α-Zearalenol
  • HY-121149
    Droloxifene
    Modulator 99.89%
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
    Droloxifene
  • HY-16023B
    (Rac)-Acolbifene
    Antagonist 98.18%
    (Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380.
    (Rac)-Acolbifene
  • HY-19464
    Org 43553
    Agonist 99.30%
    Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.
    Org 43553
  • HY-N0322S2
    Cholesterol-d6-1
    Agonist 99.01%
    Cholesterol-d6-1 is the deuterium 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-d<sub>6</sub>-1
  • HY-N2168
    Pinoresinol 4-O-β-D-glucopyranoside
    99.89%
    Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects.
    Pinoresinol 4-O-β-D-glucopyranoside
  • HY-103447R
    Zearalenone (Standard)
    Activator
    Zearalenone (Standard) is the analytical standard of Zearalenone. This product is intended for research and analytical applications. Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts.
    Zearalenone (Standard)
  • HY-138686
    GPR30 agonist-1
    Agonist 98.62%
    GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects.
    GPR30 agonist-1
  • HY-B0652
    Etonogestrel
    Agonist 99.91%
    Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel
  • HY-W011926
    Diisopropyl phthalate
    Ligand 99.37%
    Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM.
    Diisopropyl phthalate
  • HY-126351
    PROTAC ERRα ligand 2
    Antagonist 99.36%
    PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
    PROTAC ERRα ligand 2
  • HY-103457
    Y134
    Antagonist 99.67%
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.
    Y134
  • HY-147402A
    Taragarestrant meglumine
    Degrader 99.33%
    Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models.
    Taragarestrant meglumine
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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