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-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-18719A
    Endoxifen Z-isomer hydrochloride
    Inhibitor 99.67%
    Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).
    Endoxifen Z-isomer hydrochloride
  • HY-B2158
    Chlorotrianisene
    Modulator 99.02%
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
    Chlorotrianisene
  • HY-W011100
    Cyclofenil
    Modulator
    Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
    Cyclofenil
  • HY-14598S
    Diethylstilbestrol-d8
    Agonist 99.74%
    Diethylstilbestrol-d8 is the deuterium labeled Diethylstilbestrol. Diethylstilbestrol, a synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders.
    Diethylstilbestrol-d<sub>8</sub>
  • HY-N3755
    Dihydroresveratrol
    Modulator 99.41%
    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-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-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
    Inhibitor 98.92%
    PROTAC ERα Degrader-2 comprises a IAP ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
    PROTAC ERα Degrader-2
  • 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-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-14590R
    Kaempferol (Standard)
    Inhibitor 99.80%
    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-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-149295
    PROTAC ERα Degrader-4
    Degrader 99.06%
    PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
    PROTAC ERα Degrader-4
  • HY-B0141S2
    Estradiol-d5
    Agonist 99.88%
    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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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