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-175171
    Anticancer agent 276
    Inhibitor
    Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.
    Anticancer agent 276
  • HY-135581
    Raloxifene 6-glucuronide
    Modulator
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
    Raloxifene 6-glucuronide
  • HY-146267
    ERα degrader 5
    Antagonist
    ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
    ERα degrader 5
  • HY-N0322S8
    Cholesterol-18O
    Agonist
    Cholesterol-18O is the 18O-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-<sup>18</sup>O
  • HY-N6709S2
    Zeranol-d5-1
    Zeranol-d5-1 (α-Zearalanol-d5-1) is the deuterium labeled Zeranol (HY-N6709). Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
    Zeranol-d<sub>5</sub>-1
  • 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-178961
    PROTAC ERα Degrader-13
    Degrader
    PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research. (Pink: ERα Ligand (HY-12864); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W040168))
    PROTAC ERα Degrader-13
  • 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-171791
    WAY-166818
    Agonist
    WAY-166818 (WAY-818) is a synthetic nonsteroidal estrogen that is a selective agonist of ERβ.
    WAY-166818
  • 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.
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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