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-I0508S
    Phthalic acid-d4
    Antagonist 98.36%
    Phthalic acid-d4 is the deuterium labeled Phthalic acid. Phthalic acid is the final common metabolite of phthalic acid esters (PAEs). Phthalic acid can be used for the synthesis of synthetic agents, such as isophthalic acid (IPA), and terephthalic acid (TPA). Phthalic acid has applications in the preparation of phthalate ester plasticizers. Phthalic acid exhibits mutagenic effect and causes genetic damage in mammalian germ cells.
    Phthalic acid-d<sub>4</sub>
  • HY-110201
    Estrogen receptor modulator 1
    Modulator 99.91%
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
    Estrogen receptor modulator 1
  • HY-16023
    Acolbifene hydrochloride
    Antagonist 99.00%
    Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
    Acolbifene hydrochloride
  • HY-14589R
    Chrysin (Standard)
    Inhibitor
    Chrysin (Standard) is the analytical standard of Chrysin. This product is intended for research and analytical applications. Chrysin is one of the most well known estrogen blockers.
    Chrysin (Standard)
  • 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-W011927R
    4,4'-Sulfonyldiphenol (Standard)
    Antagonist
    4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
    4,4'-Sulfonyldiphenol (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-B1192R
    Estradiol benzoate (Standard)
    Agonist
    Estradiol benzoate (Standard) is the analytical standard of Estradiol benzoate. This product is intended for research and analytical applications. Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice.
    Estradiol benzoate (Standard)
  • HY-111226A
    (E/Z)-GSK5182
    Inhibitor 98.90%
    (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma.
    (E/Z)-GSK5182
  • HY-132194
    ERα degrader-2
    Inhibitor 99.71%
    ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research.
    ERα degrader-2
  • HY-B1353
    Paroxypropione
    Inhibitor 99.97%
    Paroxypropione is a manufactured, nonsteroidal estrogen which has been used medically as an antigonadotropin.
    Paroxypropione
  • HY-B0234S4
    Estrone-d2-1
    Agonist
    Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.
    Estrone-d<sub>2</sub>-1
  • HY-131404
    TPBM
    Inhibitor 98.51%
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth.
    TPBM
  • HY-B2245
    Estradiol dipropionate
    Agonist 99.46%
    Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist.
    Estradiol dipropionate
  • HY-132247B
    (S)-ErSO
    Control 99.40%
    (S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105).
    (S)-ErSO
  • HY-111061
    GTX-758
    Agonist 99.59%
    GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research.
    GTX-758
  • HY-110157
    AC-186
    Agonist 99.61%
    AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease.
    AC-186
  • HY-137004
    Indazole-Cl
    Agonist 98.72%
    Indazole-Cl (Ind-Cl) is an Estrogen receptor (ER)-β-specific agonist with inflammatory effect. Indazole-Cl inhibits cyclooxygenase-2 exression reduction induced by hypoxia. And Indazole-Cl inhibits ROS production. Indazole-Cl also inhibits cell migration and invasion by hypoxia increased by hypoxia. Indazole-Cl is potent inhibitor of hypoxia-induced inflammation in vascular smooth muscle cells (VSMCs).
    Indazole-Cl
  • HY-W010062
    4-Chlorophenylacetic acid
    Antagonist 99.97%
    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
  • HY-P5464A
    SRC-1 NR box peptide acetate
    99.63%
    SRC-1 NR box peptide acetate is a biological active peptide (This peptide is a 14-amino acid fragment from the steroid receptor cofactor SRC-1 NR II). SRC-1 NR box peptide acetate can be used to study the regulatory mechanisms of estrogen receptor ligands.
    SRC-1 NR box peptide acetate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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