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-176364
    AZD9496-O-C3-O-C3-O-C-acid
    Inhibitor
    AZD9496-O-C3-O-C3-O-C-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for ERα (HY-12870) and a PROTAC linker, which recruits E3 ligases. AZD9496-O-C3-O-C3-O-C-acid can be used for synthesis of PROTAC AZ'6421 (HY-135312).
    AZD9496-O-C3-O-C3-O-C-acid
  • HY-P11153
    HGH fragment 176-191
    Ligand
    HGH fragment 176-191 is a fragment of Human Growth Hormone. HGH fragment 176-191 binds with high affinity to Ki-67, MiB protein, and the estrogen receptor. HGH fragment 176-191 enhances the toxicity of Doxorubicin (HY-15142A)-loaded Chitosan nanoparticles against breast cancer.
    HGH fragment 176-191
  • HY-174453
    PROTAC ERα Degrader-12
    Degrader
    PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)).
    PROTAC ERα Degrader-12
  • HY-143267
    Estrogen receptor antagonist 8
    Antagonist
    Estrogen receptor antagonist 8 is a potent ER-antagonist with in vivo anti-uterotrophic potential (EC50 = 4.160 μM).
    Estrogen receptor antagonist 8
  • HY-170339
    ER ligand-5
    Ligand
    ER ligand-5 is the ligand for estrogen receptor, that can be used as ligand for target protein for PROTAC synthesis of PROTAC ERα Degrader-10 (HY-170336).
    ER ligand-5
  • HY-179232
    ERα antagonist 2
    Antagonist
    ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer.
    ERα antagonist 2
  • HY-B1192S
    Estradiol benzoate-d3
    Agonist 99.0%
    Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
    Estradiol benzoate-d<sub>3</sub>
  • HY-N6710S
    α-Zearalenol-d4
    Inhibitor
    α-Zearalenol-d4 is a deuterated labeled α-Zearalenol. 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-d<sub>4</sub>
  • HY-156125
    14-3-3σ/ERα stabilizer-1
    14-3-3σ/ERα stabilizer-1 (Compound 181) is a covalent 14-3-3σ/ERα stabilizer. 14-3-3σ/ERα stabilizer-1 can be used for research of molecular glues.
    14-3-3σ/ERα stabilizer-1
  • HY-118633
    Ethamoxytriphetol
    Modulator
    Ethamoxytriphetol (MER-25) is a nonsteroidal antiestrogen.
    Ethamoxytriphetol
  • HY-123773
    SR-16157
    Modulator
    SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC50 = 0.1 uM) and selective ERα modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research.
    SR-16157
  • HY-174475
    ER ligand-11
    Ligand
    ER ligand-11 is the ligand for ERα and can be used for synthesis of PROTACs, such as PROTAC ERα Degrader-12 (HY-174453).
    ER ligand-11
  • HY-175785
    X15695
    Degrader 98.45%
    X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer.
    X15695
  • HY-B2158S
    Chlorotrianisene-d9
    Modulator
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. 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-d<sub>9</sub>
  • HY-170332
    PROTAC ER Degrader-15
    Degrader
    PROTAC ER Degrader-15 (Compound 40) is an orally active degrader of the estrogen receptor (ER) with anticancer activity,which can be used in breast cancer research (Pink: Target Protein Ligand (HY-170334); Black: Linker (HY-30756); Blue: E3 Ligase Ligand (HY-138793); E3 Ligase Ligand-Linker Conjugate (HY-169979)).
    PROTAC ER Degrader-15
  • HY-N1556
    Psidial A
    Modulator
    Psidial A is an epimer of sesquiterpenoid-diphenylmethane meroterpenoid. Psidial A may act as a selective estrogen receptors modulator. Psidial A also has potential for anticancer research.
    Psidial A
  • HY-170341
    ER ligand-6
    ER ligand-6 is a target protein ligand of PROTAC ER Degrader-14 (HY-170340).
    ER ligand-6
  • HY-170336
    PROTAC ERα Degrader-10
    Degrader
    PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for ERα with DC50 of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model. (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))
    PROTAC ERα Degrader-10
  • HY-131586
    3,7-Dihydroxyflavone
    Modulator 98.04%
    3,7-Dihydroxyflavone (Resogalangin) is a flavonoid phytoestrogen, which can be isolated from Adenophora species. 3,7-Dihydroxyflavone is a modulator of estrogen receptors and an inhibitor of human progesterone metabolizing enzyme AKR1C1 and fungal 17β-hydroxysteroid dehydrogenase and a redox inhibitor (IC50=0.6 and 6.0 μM, respectively). 3,7-Dihydroxyflavone is a fluorescent binding substrate for human serum albumin (HSA) with excitation wavelengths of 370 nm (pH 7.4) and 350 nm (pH 3.5), respectively, and emission wavelength of 515 nm.
    3,7-Dihydroxyflavone
  • HY-124882
    Dienestrol diacetate
    Dienestrol diacetate is a synthetic nonsteroidal phenolic compound with estrogenic activity. Dienestrol diacetate can mimic the effects of estrogen in vivo, affecting the reproductive system and other related biological processes. Dienestrol diacetate is being studied for the inhibition of hormone-related diseases, such as estrogen deficiency. Dienestrol diacetate's potential applications also include possible use in hormone replacement therapy.
    Dienestrol diacetate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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