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-127133
    Methylpiperidino pyrazole
    Modulator
    Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
    Methylpiperidino pyrazole
  • HY-N2682B
    Dehydrodiconiferyl alcohol
    Agonist 98.32%
    Dehydrodiconiferyl alcohol is an estrogen receptor agonist that can promote BMP-2-induced osteoblastogenesis. Dehydrodiconiferyl alcohol also exerts anti-inflammatory activity through inactivation of NF-κB pathways.
    Dehydrodiconiferyl alcohol
  • HY-173474
    ERβ agonist-1
    Agonist
    ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer.
    ERβ agonist-1
  • HY-P3833
    Yp537
    Inhibitor
    Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor.
    Yp537
  • HY-168271
    ER ligand-2
    Degrader
    ER ligand-2 (Ligands for Target Protein for Compound 24) is the ligand of ER. ER ligand-2 can be used for synthesis PROTAC ER Degrader-11 (HY-168270).
    ER ligand-2
  • HY-146424
    OBHS
    Inhibitor
    OBHS is an estrogen receptor α (ERα) inhibitor. OBHS can also be used as a blowing agent.
    OBHS
  • HY-P991578
    SNG-8023
    Antagonist
    SNG-8023 is an anti-ERα humanized monoclonal antibody. SNG-8023 can be used for cancer research, such as breast cancer.
    SNG-8023
  • HY-145073
    PROTAC ER Degrader-10
    Inhibitor
    PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
    PROTAC ER Degrader-10
  • HY-128435
    2,4'-Dihydroxybenzophenone-1
    99.63%
    2,4'-Dihydroxybenzophenone ((Z)-SU4312) exhibited estrogenic activities. 2,4'-Dihydroxybenzophenone has oral bioactivity that can effectively protect C57BL/6J mice from Acetaminophen (HY-66005, APAP)-induced hepatotoxicity.
    2,4'-Dihydroxybenzophenone-1
  • HY-124414S
    4'-Hydroxytamoxifen-d6 (contains up to 10% E isomer)
    4'-Hydroxytamoxifen-d6 (contains up to 10% E isomer) is deuterium labeled 4'-Hydroxy Tamoxifen. 4'-Hydroxytamoxifen is a metabolite of Tamoxifen.
    4'-Hydroxytamoxifen-d<sub>6</sub> (contains up to 10% E isomer)
  • HY-B0141E
    ent-Estradiol
    Ligand
    Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC50 values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes.
    ent-Estradiol
  • HY-W746761
    Cyclodiol
    Cyclodiol is an estrogen. Cyclodiol is used for fertility control in females and also as oral contraceptives in combination with a variety of progestins.
    Cyclodiol
  • HY-181172
    FRAGHIT-4
    Inhibitor
    FRAGHIT-4 is an estrogen receptor alpha (ERα) inhibitor. FRAGHIT-4 exhibits antineoplastic activity against breast cancer via targeting ER signaling. FRAGHIT-4 can be used for the research of breast cancer.
    FRAGHIT-4
  • HY-132294A
    (1S,3R)-GNE-502
    Inhibitor
    (1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor.
    (1S,3R)-GNE-502
  • HY-N7748A
    Epi-cryptoacetalide
    Agonist
    Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2 receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities.
    Epi-cryptoacetalide
  • HY-76737S
    4-Chlorodiphenyl ether-d5
    99.3%
    4-Chlorodiphenyl ether-d5 (4-CDE-d5) is the deuterium labeled 4-Chlorodiphenyl ether. 4-Chlorodiphenyl ether is an estrogen-mimicking active compound. 4-Chlorodiphenyl ether maintains the survival of endometriotic cysts and exhibits estrogenic activity associated with the growth of endometriotic implants. 4-Chlorodiphenyl ether can be used in research related to endometriosis.
    4-Chlorodiphenyl ether-d<sub>5</sub>
  • HY-177445
    KAT6-IN-4
    Inhibitor
    KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER+/HER2- breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC).
    KAT6-IN-4
  • HY-121149B
    (E/Z)-Droloxifene
    Modulator 98.04%
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity.
    (E/Z)-Droloxifene
  • HY-A0031S2
    Bazedoxifene-d4 acetate
    Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
    Bazedoxifene-d<sub>4</sub> acetate
  • HY-162220
    HSD17B13-IN-94
    Inhibitor
    HSD17B13-IN-94 (Compound 12) is an effective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤ 0.1 μM for Estradiol (HY-B0141). HSD17B13-IN-94 can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD, NASH, or drug-induced liver injury (DILI).
    HSD17B13-IN-94
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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