1. シグナル伝達
  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.

製品番号 製品名 製品効果 純度 構造式
  • 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
  • HY-160264
    PROTAC ER Degrader-12 Degrader
    PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC50: <10 nM), and inhibits MCF-7 proliferation (DC50: <10 nM). PROTAC ER Degrader-12 has anticancer effect. Pink: ER ligand (HY-169978); Blue: E3 ligase ligand (HY-138793); Black: linker (HY-30756).
    PROTAC ER Degrader-12
  • HY-155406
    Estrogen receptor modulator 10 Antagonist
    Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research.
    Estrogen receptor modulator 10
  • HY-W554614
    Diethylstilbestrol diphosphate Agonist
    Diethylstilbestrol diphosphate (Fosfestrol) is a diphosphate of diethylstilbestrol and an agonist of estrogen receptors. Diethylstilbestrol diphosphate is a prodrug of diethylstilbestrol and has a powerful anti-gonadotropin effect. Diethylstilbestrol diphosphate can be used in the research of prostate cancer.
    Diethylstilbestrol diphosphate
  • HY-155197
    ER degrader 7 Degrader
    ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth.
    ER degrader 7
  • HY-P4689
    Prolactin-Releasing Peptide (1-31) (rat) Activator
    Prolactin-Releasing Peptide (1-31) (rat) is a UHR-1/GRP10 receptor ligand. Prolactin-Releasing Peptide (1-31) (rat) reduces fasting-induced food intake, increases plasma levels of LH, FSH, and testosterone in rats.
    Prolactin-Releasing Peptide (1-31) (rat)
  • HY-B0672S1
    Estradiol valerianate-d4 Agonist
    Estradiol valerianate-d4 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
    Estradiol valerianate-d<sub>4</sub>
  • HY-172937
    ERα degrader 13 Degrader
    ERα degrader 13 (compound MR3) is potent ERα degrader with an IC50 of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model.
    ERα degrader 13
  • HY-176956
    ER degrader 13 Degrader
    ER degrader 13 (Compound 37) is an estrogen receptor (ER) degrader. ER degrader 13 has a significant inhibitory effect on the proliferation of ER-positive breast cancer MCF-7 cells.
    ER degrader 13
  • HY-122411A
    (E/Z)-Panomifene hydrochloride Inhibitor
    (E/Z)-Panomifene (hydrochloride) is an orally active tamoxifen (TMX) (HY-13757A) analog. (E/Z)-Panomifene (hydrochloride) is a selective anti-estrogenic compound. (E/Z)-Panomifene (hydrochloride) has anti-tumor activity and can be used in breast cancer research.
    (E/Z)-Panomifene hydrochloride
  • HY-112746
    Etacstil Antagonist
    Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection.
    Etacstil
  • HY-135582S
    Raloxifene 4'-glucuronide-d4 Modulator
    Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective 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 4'-glucuronide-d<sub>4</sub>
  • HY-160856
    TOP5300 Agonist
    TOP5300 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5300 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats.
    TOP5300
  • HY-N0835R
    (20S)-Protopanaxatriol (Standard) Agonist
    (20S)-Protopanaxatriol (Standard) is the analytical standard of (20S)-Protopanaxatriol. This product is intended for research and analytical applications. (20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
    (20S)-Protopanaxatriol (Standard)
  • HY-144139
    Estrogen receptor antagonist 3 Antagonist
    Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7).
    Estrogen receptor antagonist 3
  • HY-179576
    CV2a Degrader
    CV2a is a 14-3-3-directed molecular glue-based PROTAC that selectively targets the ERα protein complex with an EC50 of 0.10 μM. CV2a cooperatively recruits VHL to the 14-3-3/ERα complex and promotes robust polyubiquitination of the 14-3-3ζ/ERα complex.
    CV2a
  • HY-135671
    AhR modulator-1 Inhibitor
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
    AhR modulator-1
  • HY-W766130
    Ethisterone-13C2
    Ethisterone-13C2 (Pregneninolone-13C2) is the 13C-labeled Ethisterone (HY-B0487). Ethisterone (Pregneninolone; 17α-Ethynyltestosterone) is a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone has almost no effect on the phagocytic activity of the reticuloendothelial system in male guinea pigs, while in utero exposure can induce abnormalities in the urogenital system of offspring.
    Ethisterone-<sup>13</sup>C<sub>2</sub>
  • HY-180852
    ER ligand-14-PEG3-Boc Ligand
    ER ligand-14-PEG3-Boc is a conjugate of a target protein ligand and linker, composed of an estrogen receptor ligand and a corresponding linker. ER ligand-14-PEG3-Boc can be used to synthesize PROTACs such as ERB-2 (HY-180850). ERB-2 exhibits good antiproliferative activity against Osimertinib (HY-15772)-resistant non-small cell lung cancer.
    ER ligand-14-PEG3-Boc
  • HY-184091
    ER ligand-15 Ligand
    ER ligand-15
製品番号 製品名 / Synonyms Species Source
製品番号 製品名 / Synonyms Application Reactivity

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