2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Estrogen Receptor/ERR

Estrogen Receptor/ERR

Estrogen Receptor/ERR

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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.

Estrogen Receptor/ERR Isoform Specific Products:

Estrogen Receptor/ERR Isoform Comparison
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 ((E)-Clomiphene-d4) hydrochloride?is a deuterium labeled Enclomiphene hydrochloride (HY-118861B). 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-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-N17632
    Moracin G
    		Inhibitor
    Moracin G is a plant-derived kinase modulator and receptor ligand that forms stable bindings with multiple key proteins (AKT1, COX2 and Estrogen receptor 1) and competitively inhibits the activity of specific kinases. By binding to MELK to disrupt cell cycle regulation, Moracin G impairs the survival and proliferation of cancer cells, induces cancer cell apoptosis, and thereby exerts anti-tumor potential. Moracin G can be used in research related to periodontitis and breast cancer.
    Moracin G
  • HY-155739
    ET receptor antagonist 3
    		Inhibitor
    ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model.
    ET receptor antagonist 3
  • HY-155738
    ET receptor antagonist 2
    		Inhibitor
    ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model.
    ET receptor antagonist 2
  • HY-175171
    Anticancer agent 276
    		Inhibitor
    Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.
    Anticancer agent 276
  • HY-138642A
    (Rac)-Vepdegestrant
    		Inhibitor
    (Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
    (Rac)-Vepdegestrant
  • HY-169063
    ZINC05925939
    		Inhibitor
    ZINC05925939 is an estrogen receptor beta (ESR2) inhibitor that can be used in breast cancer research.
    ZINC05925939
  • HY-N11787
    Cimicifuga racemosa extract
    		Inhibitor
    Cimicifuga racemosa extract is a herbal remedy with antiestrogenic properties found in the plant Cimicifuga racemosa, commonly used to alleviate menopausal symptoms and relieve symptoms such as hot flashes and night sweats.
    Cimicifuga racemosa extract
  • HY-125675
    VPC-16606
    		Inhibitor
    VPC-16606 is a selective inhibitor targeting the activation function 2 (AF2) domain of estrogen receptor α (ERα). VPC-16606 blocks the interaction between ERα and coactivators, inhibits the activity of both wild-type and clinically drug-resistant mutant ERα, and exerts inhibitory effects on hormone-resistant breast cancer cells. VPC-16606 can be used in breast cancer research.
    VPC-16606
  • HY-123163
    JNJ-1250132
    		Inhibitor
    JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM).
    JNJ-1250132
  • HY-18719BR
    Endoxifen hydrochloride (Standard)
    		Inhibitor
    Endoxifen (hydrochloride) (Standard) is the analytical standard of Endoxifen (hydrochloride). This product is intended for research and analytical applications. Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study[1][2].
    Endoxifen hydrochloride (Standard)
  • HY-19822S4
    Elacestrant-d5
    		Inhibitor
    Elacestrant-d5 (RAd1901-d5) is the deuterium labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
    Elacestrant-d<sub>5</sub>
  • HY-W673613
    ADX68692
    		Inhibitor
    ADX68692 is an orally active negative allosteric modulators of follicle-stimulating hormone receptor with a log IC50 of -5.71. ADX68692 can inhibit hCG-induced cAMP production and s ß-arrestin 2 recruitment in HEK293 cells. ADX68692 exhibits a partial effect in both mLTC-1 and primary rat Leydig cells. ADX68692 inhibits FSHR-promoted cAMP, progesterone and estradiol production. ADX68692 can reduce the number of oocytes recovered from the ampullae.
    ADX68692
  • 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-176364
    AZD9496-O-C3-O-C3-O-C-acid
    		Inhibitor
    AZD9496-O-C3-O-C3-O-C-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for ERα (HY-12870) and a PROTAC linker, which recruits E3 ligases. AZD9496-O-C3-O-C3-O-C-acid can be used for synthesis of PROTAC AZ'6421 (HY-135312).
    AZD9496-O-C3-O-C3-O-C-acid
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Estrogen Receptor/ERR Isoform Comparison

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