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-W713284
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    2-Ethylhexyl (E)-3-(4-(methoxy-d<sub>3</sub>)phenyl)acrylate
  • HY-111182
    Estrone acetate
    Activator
    Estrone acetate (Hogival) is an estrogen derivative and an estrogen receptor (ER) activator. It promotes mammary gland development, stimulates pituitary prolactin secretion, and induces the proliferation and activation of lactotrophs (e.g., by reducing prolactin storage granule size while increasing rough endoplasmic reticulum and Golgi apparatus volume density). Estrone acetate holds potential for endocrine research, particularly in studying estrogen's effects on pituitary function, prolactin regulation, and mammary tumor models.
    Estrone acetate
  • HY-142925
    ER degrader 1
    ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11).
    ER degrader 1
  • HY-160562
    PROTAC ERα Degrader-7
    Degrader
    PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha(ERα) PROTAC degrader with a DC50 value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring.
    PROTAC ERα Degrader-7
  • HY-119088
    Estrogen receptor modulator 12
    Modulator
    Estrogen receptor modulator 12 (compound 1a-(R)) is a selective estrogen receptor modulator with estrogen agonist and antagonist activities in in vivo models. Estrogen receptor modulator 12 exhibits antagonist effects on the uterus and estrogen agonist activities on bone, plasma lipids, hot flashes, and vagina in in vivo models, and is a potential compound for suppressing postmenopausal symptoms.
    Estrogen receptor modulator 12
  • HY-W777284
    Zeranol-d5 (mixture of diastereomers)
    Zeranol-d5 (mixture of diastereomers) is the deuterium labeled Zeranol (HY-N6709). Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
    Zeranol-d<sub>5</sub> (mixture of diastereomers)
  • HY-N0377R
    Liquiritigenin (Standard)
    Agonist
    Tribenoside (Standard) is the analytical standard of Tribenoside. This product is intended for research and analytical applications. Tribenoside is a vasoprotective agent, can be used for the research of hemorrhoids. Tribenoside has mild anti-inflammatory, analgesic, and wound healing properties.
    Liquiritigenin (Standard)
  • HY-143439
    LX-039
    Antagonist
    LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.
    LX-039
  • HY-164726
    Estrogen receptor modulator 11
    Modulator
    Estrogen receptor modulator 11 (Compound 27) is a tetrahydroisoquinoline derivative. Estrogen receptor modulator 11 has a certain affinity for estrogen receptors (ER), with IC50 values of 285 nM and 421 nM for ERα and ERβ, respectively. Estrogen receptor modulator 11 lacks antagonist activity in the MCF-7 cellular assay.
    Estrogen receptor modulator 11
  • HY-N0553R
    Gypenoside XVII (Standard)
    Activator
    Gypenoside XVII (Standard) is the analytical standard of Gypenoside XVII. This product is intended for research and analytical applications. Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
    Gypenoside XVII (Standard)
  • HY-142927
    ER degrader 3
    ER degrader 3 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 3 has the potential for the research of cancer diseases (extracted from patent WO2018233591A1, compound 1).
    ER degrader 3
  • HY-118242
    RU 45144
    Antagonist
    RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
    RU 45144
  • HY-A0031S
    Bazedoxifene-d4
    Modulator
    Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
    Bazedoxifene-d<sub>4</sub>
  • HY-B0487R
    Ethisterone (Standard)
    Agonist
    Ethisterone (Standard) is the analytical standard of Ethisterone. This product is intended for research and analytical applications. Ethisterone (Pregneninolone), a synthetic steroidal estrogen, is an orally active steroidal contraceptive agent. Ethisterone is reported for androgenic activity, used for the research of the gynecological disorders.
    Ethisterone (Standard)
  • HY-149105
    FSH receptor antagonist 1
    Antagonist
    FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor. FSH receptor antagonist 1 exhibits an IC50 of 28 nM on a cell line expressing the human FSH receptor. FSH receptor antagonist 1 significantly inhibits follicle growth and ovulation in an ex vivo mouse model.
    FSH receptor antagonist 1
  • HY-N3257
    Millewanin G
    Inhibitor
    Millewanin G is a prenylated isoflavonoid with antiestrogenic activity (IC50=29 μM). Millewanin G can be isolated from the leaves of M. pachycarpa cultivated in Japan.
    Millewanin G
  • HY-121351
    Inokosterone
    Inokosterone is a potential agent target of estrogen receptor 1 in rheumatoid arthritis patients.
    Inokosterone
  • HY-N1507R
    Tracheloside (Standard)
    Inhibitor
    Tracheloside (Standard) is the analytical standard of Tracheloside. This product is intended for research and analytical applications. Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.
    Tracheloside (Standard)
  • HY-106828
    E2-CDS
    E2-CDS (Estradiol 17-Dihydrotrigonelline) is a redox-based chemical delivery system for estradiol (E2). E2-CDS is capable of sustained and brain-selective delivery of estradiol.
    E2-CDS
  • HY-111845
    Estrone-N-O-C1-amido
    Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
    Estrone-N-O-C1-amido
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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