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-149833
    ERRγ inverse agonist 2
    Agonist
    ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities.
    ERRγ inverse agonist 2
  • HY-169367
    ERD-1233
    Degrader
    ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER+ breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)).
    ERD-1233
  • HY-168099
    ERα degrader 10
    Degrader
    ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer.
    ERα degrader 10
  • HY-169777
    WAY-214156
    Agonist
    WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of ERβ.
    WAY-214156
  • HY-149081
    ERα degrader 6
    Inhibitor
    ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research.
    ERα degrader 6
  • HY-B0141S5
    Estradiol-13C2
    Agonist
    Estradiol-13C2 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
    Estradiol-<sup>13</sup>C<sub>2</sub>
  • HY-107043
    7β-Hydroxy-epi-androsterone
    Modulator
    7β-Hydroxy-epi-androsterone (7β-Hydroxy-EpiA) can bind to ERβ and has anti-inflammatory and neuroprotective properties. 7β-Hydroxy-epi-androsterone is an endogenous androgenic derivative of dehydroepiandrosterone.
    7β-Hydroxy-epi-androsterone
  • HY-B0234S3
    Estrone-13C2
    Agonist
    Estrone-13C2 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[1][2].
    Estrone-<sup>13</sup>C<sub>2</sub>
  • HY-135595
    6-Raloxifene-β-D-glucopyranoside
    Antagonist
    6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
    6-Raloxifene-β-D-glucopyranoside
  • HY-127133
    Methylpiperidino pyrazole
    Modulator
    Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
    Methylpiperidino pyrazole
  • HY-N7755
    Estradiol 3-(β-D-Glucuronide) (sodium)
    Estradiol 3-(β-D-Glucuronide) sodium is the glucuronic acid derivative of estradiol (HY-B0141). Estradiol 3-(β-D-Glucuronide) sodium is radiolabeled for use in tumor imaging and biodistribution studies.
    Estradiol 3-(β-D-Glucuronide) (sodium)
  • HY-N2682B
    Dehydrodiconiferyl alcohol
    Agonist
    Dehydrodiconiferyl alcohol is an estrogen receptor agonist that can promote BMP-2-induced osteoblastogenesis. Dehydrodiconiferyl alcohol also exerts anti-inflammatory activity through inactivation of NF-κB pathways.
    Dehydrodiconiferyl alcohol
  • HY-P3833
    Yp537
    Inhibitor
    Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor.
    Yp537
  • HY-168271
    ER ligand-2
    Degrader
    ER ligand-2 (Ligands for Target Protein for Compound 24) is the ligand of ER. ER ligand-2 can be used for synthesis PROTAC ER Degrader-11 (HY-168270).
    ER ligand-2
  • HY-146424
    OBHS
    Inhibitor
    OBHS is an estrogen receptor α (ERα) inhibitor. OBHS can also be used as a blowing agent.
    OBHS
  • HY-145073
    PROTAC ER Degrader-10
    Inhibitor
    PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
    PROTAC ER Degrader-10
  • HY-128435
    2,4'-Dihydroxybenzophenone-1
    2,4'-Dihydroxybenzophenone ((Z)-SU4312) exhibited estrogenic activities. 2,4'-Dihydroxybenzophenone has oral bioactivity that can effectively protect C57BL/6J mice from Acetaminophen (HY-66005, APAP)-induced hepatotoxicity.
    2,4'-Dihydroxybenzophenone-1
  • HY-124414S
    4'-Hydroxytamoxifen-d6 (contains up to 10% E isomer)
    4'-Hydroxytamoxifen-d6 (contains up to 10% E isomer) is deuterium labeled 4'-Hydroxy Tamoxifen. 4'-Hydroxytamoxifen is a metabolite of Tamoxifen.
    4'-Hydroxytamoxifen-d<sub>6</sub> (contains up to 10% E isomer)
  • HY-132294A
    (1S,3R)-GNE-502
    Inhibitor
    (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.
    (1S,3R)-GNE-502
  • HY-N7748A
    Epi-cryptoacetalide
    Agonist
    Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2 receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities.
    Epi-cryptoacetalide
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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