estrogen receptor/err

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].

Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-selective prodrug of 17β-estradiol, which has neuroprotective effects, improves cognitive dysfunction, and can be used to study brain damage.

Estradiol 3-sulfamate (BLE 00084) is an orally active and highly potent steroidal estrone sulfatase (ES) inhibitor.Estradiol 3-sulfamate has a K(i) value of 73 nM for ES in human placental microsomes and can be used in the study of breast cancer.

Acolbifene (SCH 57068) is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.

Giredestrant tartrate (Estrogen receptor antagonist 1) is a novel, orally active, selective and effective non-steroidal estrogen receptor antagonist. Giredestrant tartrate strongly binds to ER, resulting in the failure of ER to activate the transcription of targeted genes and promoting the degradation of ER protein. Giredestrant tartrate can be used to treat tumor diseases.

Camizestrant TFA (AZD-9833 TFA) is a potent and orally active antagonist of estrogen receptor (ER).

CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

(Rac)-Acolbifene (EM-343) is the racemic form of Acolbifene. Acolbifene is a estrogen receptor antagonist. (Rac)-Acolbifene exhibits anti-estrogenic and estrogenic activities. (Rac)-Acolbifene contains a piperidine ring and exhibits good pharmacological profile,relative binding affinity (RBA)=380.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

Camizestrant (Estrogen receptor antagonist 2) is an antagonist of the estrogen receptor and can be used in studies about ER+ HER2-advanced breast cancer[1].

Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a synthetic ester, specifically the 3, 17-dipropanoyl ester, of the natural estrogen, estradiol.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.

Mestranol (Devocin), a semisynthetic estrogen, is used as an estrogen receptor agonist and must be demethylated to be biologically active.

Chrysin (5,7-Dihydroxyflavone) exhibits many biological activities and pharmacological effects, including antioxidant, anti-inflammatory, anticancer, and antiviral activities.

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

Ospemifene (FC-1271a) is a new selective non-hormonal estrogen receptor modulator (SERM) that is used for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. FDA approved on February 26, 2013.

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

Cyclofenil is an estrogen antagonist, has anti-dengue-virus activity

Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.

Avobenzone is a dibenzoylmethane endocrine disruptor that binds directly to estrogen receptor β, acting as an estrogen agonist. It is one of the most widely used filters in sunscreens for photoprotection of skin in the UV band.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

Ethisterone (17α-Ethynyltestosterone) is a progestogen hormone.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Estradiol benzoate (Benzhormovarine) is the synthetic benzoate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.

Ethynyl estradiol is a semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.

Estriol (Oestriol) is a hydroxylated metabolite of ESTRADIOL or ESTRONE that has a hydroxyl group at C3, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During PREGNANCY, a large amount of estriol is produced by the PLACENTA.

Genistin (Genistoside) is the major isoflavonoid of soybeans and soy products.It has been reported to possess various therapeutic effects, including anti-inflammatory and anticancer activities

Estrone (Aquacrine) is an aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Tamoxifen is an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM).

Octyl 4-methoxycinnamate is an organic compound that absorbs UV-B rays from the sun, protects the skin from damage, and can also be used to minimize the appearance of scars and is commonly used in cosmetics such as sunscreens and lipsticks.Octinoxate has androgenic and estrogenic effects.

Bisphenol B has a binding affinity for estrogen receptors.

beta-Estradiol 17-hemisuccinate selectively stains estrogen receptor (ER)-rich cells.

Nylestriol (LY 49825) is an agonist of estrogen receptor.

Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.