Signaling Pathway

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 Inhibitors & Modulators (46)

Product Name Catalog No. Brief Description
(20S)-Protopanaxatriol

HY-N0835

(20S)-Protopanaxatriol(g-PPT) is a metabolites of ginsenoside, protopanaxatriol (g-PPT), could modulate endothelial cell functions through the glucocorticoid receptor (GR) and oestrogen receptor (ER).

β-Estradiol 17-acetate

HY-B0708

β-Estradiol 17-acetate is a metabolite of estradiol.

β-Estradiol 17-valerate

HY-B0672

β-estradiol 17-valerate (EV) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs.

AZD9496

HY-12870

AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator(Ki=0.7 nM) and antagonist.

AZD9496 maleate

HY-12870A

AZD9496 maleate is a potent and orally bioavailable selective estrogen receptor downregulator(Ki=0.7 nM) and antagonist.

Bavachin

HY-N0233

Bavachin, a flavonoid first isolated from seeds of P.

Bazedoxifene

HY-A0031

Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.

Bazedoxifene acetate

HY-A0036

Bazedoxifene acetate (TSE 424; WAY-TES 424), a novel selective estrogen receptor modulator (SERM), has been developed to have favorable effects on bone and the lipid profile while minimizing stimulation of uterine or breast tissues.

BHPI

HY-12825

BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.

Cholesterol

HY-N0322

Cholesterol is the major sterol in mammals, and its importance in fundamental cellular processes is becoming more appreciated.

Clomiphene citrate

HY-B0463

Clomifene Citrate is a selective estrogen receptor modulator.

Dienestrol

HY-B1403

Dienestrol is a synthetic, non-steroidal estrogen, is an estrogen receptor agonist, for the treatment of menopausal and postmenopausal symptoms.

Diethylstilbestrol

HY-14598

Diethylstilbestrol, a synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders.

DPN

HY-12452

Diarylpropionitrile(DPN) is a non-steroidal estrogen receptor β(ER β) selective ligand.

DY131

HY-15483

DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.

Endoxifen E-isomer

HY-18719D

Endoxifen E-isomer is the E-isomer of (Z)-Endoxifen.

Endoxifen E-isomer hydrochloride

HY-18719C

Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).

Endoxifen hydrochloride

HY-18719B

Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor.

Endoxifen Z-isomer

HY-18719

Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).

Endoxifen Z-isomer hydrochloride

HY-18719A

Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).