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-B0845
    Prochloraz
    Antagonist 99.77%
    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
  • HY-111486
    LSZ-102
    Degrader 99.94%
    LSZ-102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with an IC50 value of 0.2 nM.
    LSZ-102
  • HY-112596
    H3B-6545
    Antagonist 99.44%
    H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
    H3B-6545
  • HY-13724B
    Pipendoxifene hydrochloride
    Modulator 99.83%
    Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer.
    Pipendoxifene hydrochloride
  • HY-143227
    DK3
    Agonist 99.82%
    DK3 is a potent and selective estrogen-related receptor alpha (ERRα) agonist.
    DK3
  • HY-N0322S1
    Cholesterol-d6
    Agonist ≥99.0%
    Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
    Cholesterol-d<sub>6</sub>
  • HY-N6625
    Chlorothalonil
    Activator 98.15%
    Chlorothalonil is a broad-spectrum foliar fungicide with oral activity. Chlorothalonil can be used to combat fungal diseases in vegetable and crop leaves. Chlorothalonil can alter the microbial community in the soil. Chlorothalonil inhibits spermatogenesis. Chlorothalonil can cause intestinal epithelial barrier dysfunction and fetal toxicity.
    Chlorothalonil
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one
    98.89%
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor proagent of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
    10β,17β-dihydroxyestra-1,4-dien-3-one
  • HY-143201
    DS20362725
    Agonist 99.34%
    DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
    DS20362725
  • HY-18719
    Endoxifen (Z-isomer)
    Inhibitor 99.20%
    Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
    Endoxifen (Z-isomer)
  • HY-112100
    PROTAC ERα Degrader-5
    Inhibitor 98.96%
    PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    PROTAC ERα Degrader-5
  • HY-12825
    BHPI
    Inhibitor ≥98.0%
    BHPI is a nuclear receptor ERα inhibitor. BHPI activates PLCγ and UPR. BHPI has antitumor activity against breast, endometrial, and ovarian cancers.
    BHPI
  • HY-B0234R
    Estrone (Standard)
    Agonist 99.88%
    Estrone (Standard) is the analytical standard of Estrone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0322S5
    Cholesterol-13C2
    Agonist 99.76%
    Cholesterol-13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
    Cholesterol-<sup>13</sup>C<sub>2</sub>
  • HY-145848
    ERRγ agonist-1
    Agonist 98.70%
    ERRγ agonist-1 is a potent ERRγ agonist. ERRγ agonist-1 increases transcriptional activities of ERRγ. ERRγ agonist-1 has the potential for the research of neuropsychological disorders.
    ERRγ agonist-1
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride
    Antagonist 99.93%
    N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
    N-Desmethyltamoxifen hydrochloride
  • HY-30270
    Mequinol
    Activator 99.98%
    Mequinol (4-Methoxyphenol)yes MercurialisOne of the bioactive ingredients, mainly used for skin discoloration. MequinolIs an antioxidant that has additive/synergistic effects on carcinogenesis when combined with other phenolic antioxidants. Mequinolalso promote hERαDependent chaperone production with potential estrogenic activity.
    Mequinol
  • HY-118716
    PhIP
    Activator 99.93%
    PhIP (2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine) is the most abundant of generation of heterocyclic amines (HCA), resulted in the cooking of meat. DNA damaging and mutagenic activities. PhIP also has oestrogenic activity that could contribute to its tissue specific carcinogenicity.
    PhIP
  • HY-B1662
    Hexestrol
    Agonist 99.89%
    Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.
    Hexestrol
  • HY-13724
    Pipendoxifene
    Modulator 99.93%
    Pipendoxifene is a selective estrogen receptor modulator (SERM).
    Pipendoxifene
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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