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-170334
    ER ligand-7
    Ligand
    ER ligand-7 is the ligand for estrogen receptor, and can be used for synthesis of PROTAC ER Degrader-15 (HY-170332) as ligand for target protein.
    ER ligand-7
  • HY-B0234S
    Estrone-13C3
    Agonist 98.0%
    Estrone-13C3 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.
    Estrone-<sup>13</sup>C<sub>3</sub>
  • HY-163680
    ERα degrader 9
    ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679).
    ERα degrader 9
  • HY-B0316S
    Avobenzone-13C,d3
    Antagonist
    Avobenzone-13C,d3 is the 13C- and deuterium labeled Avobenzone. 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-144306
    ERα degrader 4
    ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer.
    ERα degrader 4
  • HY-W716464
    Prochloraz-d7
    Prochloraz-d7 (BTS 40542-d7) is the deuterium labeled Prochloraz (HY-B0845). Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz-d<sub>7</sub>
  • HY-124414R
    4'-Hydroxytamoxifen (Standard)
    Modulator
    4'-Hydroxytamoxifen (Standard) is the analytical standard of 4'-Hydroxytamoxifen. This product is intended for research and analytical applications. 4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells.
    4'-Hydroxytamoxifen (Standard)
  • HY-135594
    4'-Raloxifene-β-D-glucopyranoside
    Antagonist
    4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
    4'-Raloxifene-β-D-glucopyranoside
  • HY-135581S1
    Raloxifene 6-glucuronide-d4 lithium
    Modulator
    Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal 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 6-glucuronide-d<sub>4</sub> lithium
  • HY-122825
    SNIPER(ER)-110
    Inhibitor
    SNIPER(ER)-110 consists of a IAP ligand and an estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively.
    SNIPER(ER)-110
  • HY-N0595R
    Genistin (Standard)
    Modulator
    Genistin (Standard) is the analytical standard of Genistin. This product is intended for research and analytical applications. Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.
    Genistin (Standard)
  • HY-108028
    NDC 1308
    NDC 1308 is an estradiol analogue. NDC 1308 can bind estrogen receptor beta and inhibit cancer cell proliferation by blocking chromosome replication. NDC 1308 can be used for the research of cancer, such as breast cancer.
    NDC 1308
  • HY-100266
    Nitromifene
    Antagonist
    Nitromifene is an antagonist of estrogen receptor (ER).
    Nitromifene
  • HY-D2280
    Estrogen receptor β/HDAC probe 1
    Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC.
    Estrogen receptor β/HDAC probe 1
  • HY-B1623R
    Cyproterone (Standard)
    Cyproterone (Standard) is the analytical standard of Cyproterone. This product is intended for research and analytical applications. Cyproterone is an antiandrogen that suppresses the actions of testosterone via blocking androgen receptors. Cyproterone’s acetate form can be used in the research of hypersexuality and prostate cancer.
    Cyproterone (Standard)
  • HY-106056
    Zindoxifene
    Agonist
    Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer.
    Zindoxifene
  • HY-19822S2
    Elacestrant-d10
    Degrader
    Elacestrant-d10 is the deuterium labeled of 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 also inhibits growth of ER+ breast cancer cell lines in vitro and in vivo.
    Elacestrant-d<sub>10</sub>
  • HY-122359B
    Levormeloxifene fumarate
    Modulator
    Levormeloxifene (fumarate) is a stable salt form of Levormeloxifene. Levormeloxifene (fumarate) is an estrogen receptor modulator that plays an important role in prevention of postmenopausal bone loss.
    Levormeloxifene fumarate
  • HY-N0233R
    Bavachin (Standard)
    Agonist
    Bavachin (Standard) is the analytical standard of Bavachin. This product is intended for research and analytical applications. Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
    Bavachin (Standard)
  • HY-160563
    PROTAC ERα Degrader-8
    Degrader
    PROTAC ERα Degrader-8 (compound ii-56) is a potent PROTAC degrader of Erα, with DC50 of 0.000006 μM in MCF7 cells.
    PROTAC ERα Degrader-8
Cat. No. Product Name / Synonyms Species Source
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