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Estrogen Receptor/ERR

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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.

Products Related to Estrogen Receptor/ERR(175)

  • GC62723 structure
    GC62723ARV-471
    CAS: 2229711-68-4
    Purity: >99.50%

    ARV-471 is an orally bioavailable estrogen receptor-targeted (ER-targeted) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

  • GC63185 structure
    GC63185Segetalin B
    CAS: 164991-89-3
    Purity: >99.50%

    Segetalin B, a cyclopentapeptide from Vaccaria segetalis, possesses estrogen-like activity.

  • GC63329 structure
    GC63329Toremifene-d6 citrate
    CAS: 1246833-71-5
    Purity: >98%
  • GC63464 structure
    GC63464Rintodestrant
    CAS: 2088518-51-6
    Purity: >98%

    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.

  • GC63643 structure
    GC63643Estradiol-d4
    CAS: 66789-03-5
    Purity: >99.50%

    Estradiol-d4 (β-Estradiol-d4) is the deuterium labeled Estradiol.

  • GC63843 structure
    GC63843Cholesterol-13C3
    Purity: >98%
  • GC63899 structure
    GC63899hFSH-β-(33-53) (TFA)
    Purity: >98%
  • GC63988 structure
    GC63988DK1
    CAS: 1187568-17-7
    Purity: >99.00%

    DK1 is a potent modulator of estrogen related receptor.

  • GC63989 structure
    GC63989DK3
    CAS: 1187568-16-6
    Purity: >98%

    DK3 is a potent and selective estrogen-related receptor alpha (ERRα) agonist.

  • GC64334 structure
    GC64334Cholesterol-13C5
    CAS: 150044-24-9
    Purity: >98%
  • GC64345 structure
    GC64345OP-1074
    CAS: 1443752-76-8
    Purity: >99.00%

    OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2?nM, respectively.

  • GC64350 structure
    GC64350PROTAC ER Degrader-4
    CAS: 2361114-15-8
    Purity: >98.00%

    PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.

  • GC64437 structure
    GC64437Estrone-d4
    CAS: 53866-34-5
    Purity: >98.00%
  • GC64453 structure
    GC64453GSK5182
    CAS: 877387-37-6
    Purity: >98.00%

    GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM.

  • GC64477 structure
    GC64477Cholesterol-13C2
    CAS: 78887-48-6
    Purity: >98.00%

    Cholesterol-13C2 is a 13C-labeled cholesterol.

  • GC64533 structure
    GC64533DS45500853
    CAS: 2735803-28-6
    Purity: >98%

    DS45500853 is an estrogen-related receptor α (ERRα) agonist.

  • GC64652 structure
    GC64652DS20362725
    CAS: 2735803-20-8
    Purity: >98.00%

    DS20362725 is an estrogen-related receptor α (ERRα) agonist.

  • GC65590 structure
    GC65590GNE-502
    CAS: 1953134-16-1
    Purity: >99.00%

    GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.

  • GC65606 structure
    GC65606GNE-274
    CAS: 2369048-69-9
    Purity: >98.00%

    GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines.?GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research.

  • GC65609 structure
    GC65609Glicoricone
    CAS: 161099-37-2
    Purity: >96.00%

    Glicoricone, a phenolic compound, is isolated from a species of licorice.

  • GC65885 structure
    GC65885(1S,3R)-GNE-502
    CAS: 1953134-15-0
    Purity: >98%

    (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.

  • GC66878 structure
    GC66878Estradiol enanthate
    CAS: 4956-37-0
    Purity: >98%

    Estradiol enanthate is a shorter-acting estrogen. The combination of Estradiol enanthate and dihydroxyprogesterone acetophenide can be used as a monthly injectable contraceptive.

  • GC67695 structure
    GC67695Taragarestrant meglumine
    CAS: 2446618-18-2
    Purity: >98%
  • GC67927 structure
    GC67927ERα degrader-2
    CAS: 2235396-63-9
    Purity: >99.00%