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-13757A
    Tamoxifen
    		Modulator 99.92%
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen
  • HY-B0141
    Estradiol
    		Agonist 99.93%
    Estradiol (β-Estradiol) is a steroid hormone and the major female sex hormone. Estradiol can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering.
    Estradiol
  • HY-16950
    4-Hydroxytamoxifen
    		Modulator 99.96%
    4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation.
    4-Hydroxytamoxifen
  • HY-13636
    Fulvestrant
    		Antagonist 99.95%
    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
  • HY-N0322
    Cholesterol
    		Agonist 99.94%
    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
  • 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-161742
    Fumagilin-105
    Fumagilin-105 is an autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization with DC50 values of 0.7 μM for MetAP2 in HEK293 cells.
    Fumagilin-105
  • HY-161740
    PHTPP-1304
    		Degrader 99.96%
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization and degradation of estrogen receptor ERβ (DC50:~2 nM, HEK293T). PHTPP-1304 also induces the formation of p62+ERβ+ puncta that are affected by autophagic flux in a dose-dependent manner.
    PHTPP-1304
  • HY-14590
    Kaempferol
    		Inhibitor 99.92%
    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
  • HY-103449
    G15
    		Antagonist ≥99.0%
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
    G15
  • HY-13757
    Tamoxifen Citrate
    		Modulator 99.93%
    Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen Citrate
  • HY-107216
    G-1
    		Agonist 99.76%
    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
    G-1
  • HY-138642
    Vepdegestrant
    		Inhibitor 99.60%
    Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
    Vepdegestrant
  • HY-19822
    Elacestrant
    		Inhibitor 99.80%
    Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
    Elacestrant
  • HY-N2371
    27-Hydroxycholesterol
    		Modulator 99.74%
    27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.
    27-Hydroxycholesterol
  • HY-B0234
    Estrone
    		Agonist 99.86%
    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
  • HY-103456
    PHTPP
    		Antagonist 99.70%
    PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα.
    PHTPP
  • HY-100689
    Propyl pyrazole triol
    		Agonist 99.11%
    Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
    Propyl pyrazole triol
  • HY-B1192
    Estradiol benzoate
    		Agonist 99.89%
    Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice.
    Estradiol benzoate
  • HY-14589
    Chrysin
    		Inhibitor 99.85%
    Chrysin is one of the most well known estrogen blockers.
    Chrysin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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