2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Related Products

PDF 3.53 MB

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-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-182498
    (Z)-Norendoxifen
    		Modulator
    (Z)-Norendoxifen is an aromatase inhibitor and estrogen receptor modulator. The IC50 value of (Z)-Norendoxifen against aromatase is 102 nM. The EC50 values of (Z)-Norendoxifen for ER-α and ER-β are 27.0 nM and 35.2 nM, respectively. (Z)-Norendoxifen can be used in breast cancer research.
    (Z)-Norendoxifen
  • 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-176955
    ER degrader 12
    		Degrader
    ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC50 values for ERα and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC50 of 1.53 nM. ER degrader 12 can be used for research on breast cancer.
    ER degrader 12
  • 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-183804
    PROTAC ER Degrader-16
    		Degrader
    PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC50 of 1.4 nM and an IC50 of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research.
    PROTAC ER Degrader-16
  • HY-135529
    Trioxifene
    		Modulator
    Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma.
    Trioxifene
  • 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-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
  • HY-114631
    EM-800
    		Antagonist
    EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism.
    EM-800
  • HY-170377
    ER degrader 10
    		Degrader
    ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model.
    ER degrader 10
  • HY-B0723S
    Ospemifene-d4
    		Modulator 99.65%
    Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
    Ospemifene-d<sub>4</sub>
  • HY-A0287A
    Clomiphene hydrochloride
    		Inhibitor
    Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) hydrochloride is an orally active ovulation-inducing agent. Clomiphene hydrochloride binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene hydrochloride can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene hydrochloride ameliorates memory impairment in PCOS models. Clomiphene hydrochloride mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene hydrochloride can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer.
    Clomiphene hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.