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-145572A
    Imlunestrant tosylate
    Degrader 98.54%
    Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC).
    Imlunestrant tosylate
  • HY-125263
    OP-1074
    Degrader 99.77%
    OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
    OP-1074
  • HY-B0412S2
    Estriol-d3
    Antagonist
    Estriol-d3 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
    Estriol-d<sub>3</sub>
  • HY-113251S
    2-Hydroxyestrone-d4
    Inhibitor
    2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
    2-Hydroxyestrone-d<sub>4</sub>
  • HY-A0036B
    Bazedoxifene (acetate)-B
    Bazedoxifene (acetate)-B (TSE-424 (acetate)-B) is the B-crystal form compound of Bazedoxifene acetate (HY-A0036). Bazedoxifene acetate is an orally active, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively.
    Bazedoxifene (acetate)-B
  • HY-135312
    AZ'6421
    Inhibitor 98.13%
    AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
    AZ'6421
  • HY-145716
    Nafoxidine
    Antagonist 98.70%
    Nafoxidine, a nonsteroidal estrogen antagonist, is shown to possess antitumor activity against breast cancer.
    Nafoxidine
  • HY-18719D
    Endoxifen (E-isomer)
    Inhibitor 98.02%
    Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer exhibits antiestrogenic effects.
    Endoxifen (E-isomer)
  • HY-145556
    Bexirestrant
    Inhibitor 99.46%
    Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.
    Bexirestrant
  • HY-B1830
    Estradiol enanthate
    99.41%
    Estradiol enanthate (E2EN) is a shorter-acting estrogen. Estradiol enanthate is an injectable contraceptive in combination with Dihydroxyprogesterone acetophenide. Estradiol enanthate promotes withdrawal bleeding, in a pattern similar to menstruation.
    Estradiol enanthate
  • HY-13757AS
    Tamoxifen-d5
    Modulator 99.99%
    Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
    Tamoxifen-d<sub>5</sub>
  • HY-N1507
    Tracheloside
    Inhibitor 99.77%
    Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.
    Tracheloside
  • HY-124414
    4'-Hydroxytamoxifen
    Modulator 99.2%
    4'-Hydroxytamoxifen is a metabolite of Tamoxifen. 4'-Hydroxytamoxifen shows higher affinity for the ER than Tamoxifen. 4'-Hydroxytamoxifen induces a non-apoptotic cytotoxic effect in human endometrial adenocarcinoma cells.
    4'-Hydroxytamoxifen
  • HY-B0412R
    Estriol (Standard)
    Antagonist
    Estriol (Standard) is the analytical standard of Estriol. This product is intended for research and analytical applications.
    Estriol (Standard)
  • HY-D0272
    2,3,4-Trihydroxybenzophenone
    99.92%
    2,3,4-Trihydroxybenzophenone is a hydroxylated benzophenone UV filter with estrogenic activity. 2,3,4-Trihydroxybenzophenone is a quorum sensing inhibitor and an EC 1.14.18.1 (tyrosinase) inhibitor. 2,3,4-Trihydroxybenzophenone is also a human urinary metabolite, a rat metabolite and a drug metabolite.
    2,3,4-Trihydroxybenzophenone
  • HY-13636S
    Fulvestrant-d3
    Antagonist
    Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
    Fulvestrant-d<sub>3</sub>
  • HY-128838
    PROTAC ERRα Degrader-1
    Inhibitor 98.22%
    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
    PROTAC ERRα Degrader-1
  • HY-B0141S3
    Estradiol-d2
    Agonist 99.44%
    Estradiol-d2 is the deuterium 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.
    Estradiol-d<sub>2</sub>
  • HY-B0216S
    Ethynyl Estradiol-d4
    Agonist 99.00%
    Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 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-d<sub>4</sub>
  • HY-N4121
    Isocurcumenol
    Inhibitor 99.47%
    Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1μg/mL and 178.2 μg/mL in DLA and KB cells, respectively.
    Isocurcumenol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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