1. Vitamin D Related/Nuclear Receptor
  2. 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.

Estrogen Receptor/ERR Related Products (371):

Cat. No. Product Name Effect Purity
  • HY-B0141
    Estradiol Agonist 99.99%
    Estradiol (β-Estradiol) is a steroid hormone and the major female sex hormone. Estradiol can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering[1][2].
  • HY-16950
    4-Hydroxytamoxifen Modulator 99.96%
    4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) induces CRISPR/Cas9 systems based on ER mediated nucleus translocation[1][2][3][4].
  • HY-13636
    Fulvestrant Antagonist
    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[1].
  • HY-N0322
    Cholesterol Agonist
    Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3].
  • HY-13757A
    Tamoxifen Modulator 99.92%
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively[5]. Tamoxifen activates autophagy and induces apoptosis[4]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[6].
  • HY-13757S
    Tamoxifen-d3 hydrochloride Modulator
    Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[5]. Tamoxifen Citrate activates autophagy and induces apoptosis[4].Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse[6].
  • HY-135582S
    Raloxifene 4'-glucuronide-d4 Modulator
    Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
  • 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[1].
  • HY-B0141S
    Estradiol-d3 Agonist 98.60%
    Estradiol-d3 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.
  • 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)[1].
  • 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[1].
  • HY-101119
    GLL398 Inhibitor
    GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models[1].
  • HY-B1361
    Estropipate Agonist 98.94%
    Estropipate is a form of estrogen, used to treat symptoms of menopause, also used to prevent osteoporosis.
  • HY-U00216
    NNC45-0781 Agonist
    NNC45-0781 is a tissue-selective estrogen partial-agonist.
  • HY-128839
    PROTAC ERRα Degrader-2 Inhibitor
    PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader[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.
  • HY-B1617AS1
    Zuclomiphene-d5 citrate
    Zuclomiphene-d5 (citrate) is the deuterium labeled Zuclomiphene citrate[1]. Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent[2][3][4][5].
  • 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[1].
  • HY-161253
    OSU-ERb-12 Agonist
    OSU-ERb-12 is a ERβ agonist, and suppress ovarian cancer cell proliferation in vitro and in vivo. OSU-ERb-12 decreases the expression of Snail[1][2].
  • HY-B0672R
    Estradiol valerate (Standard) Agonist 99.87%
    Estradiol valerianate (Standard) is the analytical standard of Estradiol valerianate. This product is intended for research and analytical applications. Estradiol valerate (β-Estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.