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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.

Estrogen Receptor/ERR Related Products (101):

Cat. No. Product Name Effect Purity
  • HY-13757A
    Tamoxifen Modulator 99.76%
    Tamoxifen is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
  • HY-13636
    Fulvestrant Inhibitor 99.99%
    Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.
  • HY-B0141
    Estradiol Agonist 99.99%
    Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
  • HY-16950
    4-Hydroxytamoxifen Modulator 99.86%
    4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
  • HY-13757
    Tamoxifen Citrate Inhibitor >99.0%
    Tamoxifen Citrate is a selective estrogen receptor modulator (SERM).
  • HY-103449
    G15 Antagonist >99.0%
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  • HY-100689
    Propyl pyrazole triol Agonist >99.0%
    Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
  • HY-111846
    PROTAC ERα Degrader-2 Inhibitor 98.02%
    PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
  • HY-19822A
    Elacestrant dihydrochloride Inhibitor 98.93%
    Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-12870
    AZD9496 Antagonist 99.15%
    AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM.
  • HY-103456
    PHTPP Antagonist 99.07%
    PHTPP is a selective ERβ antagonist.
  • HY-A0036
    Bazedoxifene acetate Modulator 99.93%
    Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
  • HY-10426
    XCT790 Antagonist 98.01%
    XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
  • HY-107216
    G-1 Agonist 99.20%
    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
  • HY-N2371
    27-Hydroxycholesterol Modulator 99.38%
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-13738A
    Raloxifene hydrochloride Antagonist 99.94%
    Raloxifene hydrochloride(LY156758 hydrochloride) is a second generation selective estrogen receptor antagonist.
  • HY-B0234
    Estrone Agonist 99.86%
    Estrone is an estrogenic hormone.
  • HY-14590
    Kaempferol Inhibitor 99.47%
    Kaempferol inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK.
  • HY-N0322
    Cholesterol Agonist >98.0%
    Cholesterol is the major sterol in mammals, and its importance in fundamental cellular processes is becoming more appreciated.
  • HY-B1192
    Estradiol benzoate Agonist 99.69%
    Estradiol Benzoate, a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
Isoform Specific Products

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