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-122359A
    rel-Levormeloxifene
    Modulator
    rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells.
    rel-Levormeloxifene
  • HY-B1630
    Stilbestrol dipropionate
    Stilbestrol dipropionate is an estrogen-like compound with hormone suppressive activity for recurrent prostate cancer. Stilbestrol dipropionate can be used to suppress diseases associated with estrogen deficiency.
    Stilbestrol dipropionate
  • HY-168270
    PROTAC ER Degrader-11
    Degrader
    PROTAC ER Degrader-11 (Example 26-1) is a potent PROTAC ER degrader, with the IC50 of 0.66 nM. PROTAC ER Degrader-11 plays an important role in cancer research(Sturcture Note:(Blue: Cereblon ligand (HY-W797329), Black: linker (HY-W262798);Pink: ER ligand (HY-168271)).
    PROTAC ER Degrader-11
  • HY-155492
    ERα degrader 7
    Degrader
    ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research.
    ERα degrader 7
  • HY-122411
    Panomifene
    Inhibitor
    Panomifene (EGIS 5650) is a tamoxifen (HY-13757A) analog with an antiestrogenic activity. Panomifene can be used in the research of breast cancer.
    Panomifene
  • HY-103453
    (R)-DPN
    Chemical
    (R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively.
    (R)-DPN
  • HY-103452
    RU58668
    Antagonist
    RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research.
    RU58668
  • HY-135582
    Raloxifene 4'-glucuronide
    Modulator
    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
  • HY-N6714R
    Alternariol (Standard)
    Activator
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol (Standard)
  • HY-B1012R
    Quinestrol (Standard)
    Agonist
    Quinestrol (Standard) is the analytical standard of Quinestrol. This product is intended for research and analytical applications. Quinestrol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Quinestrol (Standard)
  • HY-107803
    Geranium oil
    Agonist
    Geranium oil serves as a partial agonist for estrogen receptor (ER), enhancing both the cytotoxicity induced by Tamoxifen (TMX) (HY-13757A) in GT1-7 cells and the adverse effects of TMX on the central nervous system. Geranium oil can be utilized in the research of neurological disorders such as dementia.
    Geranium oil
  • HY-146440
    LSD1/ER-IN-1
    Inhibitor
    LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM.
    LSD1/ER-IN-1
  • HY-126932
    TTC-352
    Agonist
    TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites.
    TTC-352
  • HY-153700
    Estrogen receptor modulator 8
    Inhibitor
    Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM.
    Estrogen receptor modulator 8
  • HY-W009301R
    6-Ketoestradiol (Standard)
    6-Ketoestradiol (Standard) is the analytical standard of 6-Ketoestradiol. This product is intended for research and analytical applications. 6-Ketoestradiol can be used to synthesize re-containing 7α-substituted estradiol complexes.
    6-Ketoestradiol (Standard)
  • HY-W106688
    Triisopropyl phosphate
    Antagonist
    Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression, exhibits anti-estrogenic activity that inhibits Estradiol (HY-B0141)-induced MCF-7 cell proliferation with an EC50 of 341 μM. Triisopropyl phosphate inhibits the estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM.
    Triisopropyl phosphate
  • HY-B0316R
    Avobenzone (Standard)
    Antagonist
    Avobenzone (Standard) is the analytical standard of Avobenzone. This product is intended for research and analytical applications. Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
    Avobenzone (Standard)
  • HY-123047S
    Tibolone-d5
    Agonist
    Tibolone-d5 is deuterium labeled Tibolone. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
    Tibolone-d<sub>5</sub>
  • HY-W114419
    Bisphenol C
    Activator ≥98.0%
    Bisphenol C is an ERα agonist and ERβ antagonist that inhibits 17β-estradiol.
    Bisphenol C
  • HY-19822S1
    Elacestrant-d4-1
    Inhibitor
    Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
    Elacestrant-d<sub>4</sub>-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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