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-128527
    PROTAC ER Degrader-3
    Inhibitor
    PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    PROTAC ER Degrader-3
  • HY-145071
    PROTAC ERα Y537S degrader-1
    Inhibitor
    PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader.
    PROTAC ERα Y537S degrader-1
  • HY-19822S3
    Elacestrant-d6
    Inhibitor
    Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER+ breast cancer cell lines both in vitro and in vivo.
    Elacestrant-d<sub>6</sub>
  • HY-118861S
    Enclomiphene-d4 hydrochloride
    Inhibitor ≥99.0%
    Enclomiphene-d4 hydrochloride is a deuterium labeled Enclomiphene hydrochloride. Enclomiphen hydrochloride is a potent and orally active estrogen receptor antagonist with antioestrogenic property.
    Enclomiphene-d<sub>4</sub> hydrochloride
  • HY-132294
    GNE-502
    Inhibitor 99.73%
    GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.
    GNE-502
  • HY-128528
    PROTAC ER Degrader-2
    Inhibitor
    PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    PROTAC ER Degrader-2
  • HY-114411
    ERRγ inverse agonist 1
    Antagonist
    ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC50 of 40 nM.
    ERRγ inverse agonist 1
  • HY-135903
    Giredestrant tartrate
    Antagonist
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
    Giredestrant tartrate
  • HY-144138
    Estrogen receptor antagonist 2
    Antagonist
    Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3).
    Estrogen receptor antagonist 2
  • HY-W010062R
    4-Chlorophenylacetic acid (Standard)
    Antagonist
    4-Chlorophenylacetic acid (Standard) is the analytical standard of 4-Chlorophenylacetic acid. This product is intended for research and analytical applications. 4-Chlorophenylacetic acid is a halogenated phenylacetic acid derivative. 4-Chlorophenylacetic acid is a potent aromatase inhibitor and antagonizes estrogen signaling. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp. strain CBS3. 4-Chlorophenylacetic acid is effective against estrogen-induced mammary tumorigenesis.
    4-Chlorophenylacetic acid (Standard)
  • HY-129619
    SNIPER(ER)-87
    Modulator
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
    SNIPER(ER)-87
  • HY-13738S
    Raloxifene-d4
    Modulator
    Raloxifene-d4 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
    Raloxifene-d<sub>4</sub>
  • HY-B1176S
    Equilin-d4
    Agonist
    Equilin-d4 is the deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism.
    Equilin-d<sub>4</sub>
  • HY-B1662S
    (Rac)-Hexestrol-d4
    (Rac)-Hexestrol-d4 is the deuterium labeled (Rac)-Hexestrol.
    (Rac)-Hexestrol-d<sub>4</sub>
  • HY-B0672S
    Estradiol valerianate-d9
    Agonist
    Estradiol valerianate-d9 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
    Estradiol valerianate-d<sub>9</sub>
  • HY-13738S2
    Raloxifene-d4 hydrochloride
    Modulator
    Raloxifene-d4 (hydrochloride) is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
    Raloxifene-d<sub>4</sub> hydrochloride
  • HY-B1662S1
    (Rac)-Hexestrol-d6
    (Rac)-Hexestrol-d6 is the deuterium labeled (Rac)-Hexestrol.
    (Rac)-Hexestrol-d<sub>6</sub>
  • HY-155737
    ET receptor antagonist 1
    Inhibitor
    ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model.
    ET receptor antagonist 1
  • HY-121094
    Androgen receptor allosteric antagonist 1
    Antagonist
    Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer.
    Androgen receptor allosteric antagonist 1
  • HY-B0216S2
    Ethynyl Estradiol-13C2
    Agonist
    Ethynyl Estradiol-13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Ethynyl Estradiol-<sup>13</sup>C<sub>2</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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