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-N0587R
    Demethylzeylasteral (Standard)
    Modulator
    Demethylzeylasteral (Standard) is the analytical standard of Demethylzeylasteral. This product is intended for research and analytical applications. Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation .
    Demethylzeylasteral (Standard)
  • HY-107906
    Conjugated estrogen sodium
    Conjugated estrogen sodium is a medication composed of a blend of estrogen hormones, utilized in the treatment of moderate to severe hot flashes, vaginal changes, and various other symptoms associated with menopause or decreased estrogen levels.
    Conjugated estrogen sodium
  • HY-138642A
    (Rac)-Vepdegestrant
    Inhibitor
    (Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) 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.
    (Rac)-Vepdegestrant
  • HY-161692
    ERα degrader 8
    Degrader
    ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC50 value of 0.15 μM.
    ERα degrader 8
  • HY-163755
    GPER activator 1
    GPER activator 1 (compound 6-26) is a GPER-selective compound without cytotoxicity. GPER activator 1 exhibits dual inhibition of TNFα- and IL-6-induced inflammation.
    GPER activator 1
  • HY-P10843
    R4K1
    Modulator
    R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer.
    R4K1
  • HY-129099
    N-Desmethyltamoxifen
    Antagonist
    N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
    N-Desmethyltamoxifen
  • HY-123664
    Trioxifene mesylate
    Trioxifene mesylate (LY133314) is an antiestrogenic compound. Trioxifene mesylate elicits mixed agonist-antagonist actions on estrogen target tissues.
    Trioxifene mesylate
  • HY-153478
    Estrogen receptor modulator 7
    Modulator
    Estrogen receptor modulator 7 is a potent estrogen receptor modulator. Estrogen receptor modulator 7 can be used in research of cancer.
    Estrogen receptor modulator 7
  • HY-142926
    ER degrader 2
    ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1).
    ER degrader 2
  • HY-169063
    ZINC05925939
    Inhibitor
    ZINC05925939 is an estrogen receptor beta (ESR2) inhibitor that can be used in breast cancer research.
    ZINC05925939
  • HY-B0005AS
    Toremifene-d6
    Modulator
    Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
    Toremifene-d<sub>6</sub>
  • HY-14598S1
    Diethylstilbestrol-d3
    Agonist
    Diethylstilbestrol-d3 is deuterium labeled Diethylstilbestrol.
    Diethylstilbestrol-d<sub>3</sub>
  • HY-N8170
    4',2-Dihydroxy-4,6-dimethoxydihydrochalcone
    Agonist
    4',2-Dihydroxy-4,6-dimethoxydihydrochalcone, an estrogen agonist, shows binding affinity for bovine uterine estrogen receptor with an IC5050 of 15 μM.
    4',2-Dihydroxy-4,6-dimethoxydihydrochalcone
  • HY-167701
    OBHSA
    Degrader
    OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders.
    OBHSA
  • HY-120207
    (R)-GDC-0927
    Antagonist 98.78%
    (R)-GDC-0927 ((R)-SRN-927) is a (R)-enantiomer of GDC-0927 (HY-111484).
    (R)-GDC-0927
  • HY-118861
    Enclomiphene
    Antagonist
    Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.
    Enclomiphene
  • HY-N11787
    Cimicifuga racemosa extract
    Inhibitor
    Cimicifuga racemosa extract is a herbal remedy with antiestrogenic properties found in the plant Cimicifuga racemosa, commonly used to alleviate menopausal symptoms and relieve symptoms such as hot flashes and night sweats.
    Cimicifuga racemosa extract
  • HY-144137
    Estrogen receptor antagonist 1
    Antagonist
    Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4).
    Estrogen receptor antagonist 1
  • HY-168101
    ERα degrader 11
    Degrader
    ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells.
    ERα degrader 11
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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