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-N6710
    α-Zearalenol
    Inhibitor 99.73%
    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-164764
    ADX61623
    Inhibitor 98.84%
    ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease.
    ADX61623
  • 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-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-112100
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1
    Inhibitor 99.18%
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. MC-Val-Cit-PAB-PROTAC ERα Degrader-1 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    MC-Val-Cit-PAB-PROTAC ERα Degrader-1
  • HY-18719A
    Endoxifen Z-isomer hydrochloride
    Inhibitor 99.67%
    Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer hydrochloride inhibits PKCβ1 kinase activity. Endoxifen Z-isomer hydrochloride attenuates PKCβ1-activated AKTSer473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer hydrochloride exhibits anticancer activity against hormone-resistant metastatic breast cancer.
    Endoxifen Z-isomer hydrochloride
  • HY-N7627
    Regaloside C
    Inhibitor 99.62%
    Regaloside C is an anti-inflammatory agent and antioxidant that scavenges ABTS and DPPH free radicals. Regaloside C targets multiple molecules including TNF-α, MMP-2, ERα, AKT1, TLR4 and HSP90-α. Regaloside C is applicable to research related to inflammatory diseases.
    Regaloside C
  • HY-113251
    2-Hydroxyestrone
    Inhibitor 98.57%
    2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
    2-Hydroxyestrone
  • HY-112611
    H3B-5942
    Inhibitor 98.25%
    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-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-41570
    3-Formylsalicylic acid
    Inhibitor 98.46%
    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-135312
    AZ'6421
    Inhibitor 98.13%
    AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
    AZ'6421
  • HY-N4121
    Isocurcumenol
    Inhibitor 99.47%
    Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1μg/mL and 178.2 μg/mL in DLA and KB cells, respectively.
    Isocurcumenol
  • 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-159613
    PELP1-IN-1
    Inhibitor 99.28%
    PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER+ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer.
    PELP1-IN-1
  • HY-113251S
    2-Hydroxyestrone-d4
    Inhibitor
    2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
    2-Hydroxyestrone-d<sub>4</sub>
  • HY-145556
    Bexirestrant
    Inhibitor 99.46%
    Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.
    Bexirestrant
  • 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-128838
    PROTAC ERRα Degrader-1
    Inhibitor 98.22%
    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
    PROTAC ERRα Degrader-1
  • HY-137391
    2-Bromoestradiol
    Inhibitor 99.59%
    2-Bromoestradiol is a estrogen 2-hydroxylase inhibitor. 2-Bromoestradiol decreases irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins.
    2-Bromoestradiol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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