estrogen receptor/err

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

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 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β with a remarkable affinity (K i = 0.44 nM). This compound exhibits an impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

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].

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 Antagonist 4 is a potent inhibitor of the estrogen receptor (ER), crucial for regulating cell growth, differentiation, and apoptosis. This compound holds promise for cancer research[1].

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signalling systems play an important role in the regulation of cell growth, differentiation and apoptosis, and Estrogen receptor antagonist 4 has shown potential for research into cancer diseases.

Estrogen receptor antagonist 5 is a potent antagonist of the Estrogen receptor. Estrogen receptor (Estrogen receptor) is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. estrogen receptor antagonist 5 has potential for metastatic disease studies.

Estrogen Receptor Antagonist 7 (Compound 13) is a potent antagonist of estrogen receptors (ER), demonstrating antiproliferative effects against breast and ovarian cancer cells, along with anticancer and anti-uterotrophic activities [1].

Estrogen receptor antagonist 2 is a selective down-regulator of estrogen receptor. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. estrogen receptor antagonist 2 has research potential for breast cancer disease.

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

Estrogen receptor α antagonist 1 (compound 35) is a highly selective estrogen receptor α antagonist that acts on estrogen receptor α (IC50: 0.02 μM), estrogen receptor β (IC50. Estrogen receptor α antagonist 1 (compound 35) can be used to study tumours.

Estrogen receptor antagonist 1 is a potent antagonist of the estrogen receptor. Estrogen receptor antagonist 1 has shown research potential in breast cancer disease.

Estrogen receptor-IN-1 (compound 16) is an effective estrogen receptor (ER) inhibitor with IC 50 s of 13, 5μM for ERα and Erβ, respectively [1].

Estrogen receptor β antagonist 2 is a selective, potent estrogen receptor β (ERβ) antagonist that acts on Erα (IC50: 109.10 μM) and Erβ (IC50: 0.63 μM).

Estrogen receptor antagonist 6 is a potent antagonist of the Estrogen receptor. Estrogen receptor is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. Compound 166).

ARV-471 (Vepdegestrant) is a orally active Cereblon -based estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.

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.

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.

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

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.

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

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).

4,4'-Iminodiphenol (Leucoindophenol) is an inactive estrogen receptor ligand with a diphenylamine backbone.

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

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

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.

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

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.

Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).

(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.

Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6 GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.

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.

(E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.

kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activation.

Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.

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

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.

Bavachin (Corylifolin) is a phytoestrogen that activates the estrogen receptors ERα and ERβ.

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.

Dienestrol (Restrol) is a synthetic and nonsteroidal estrogen, which is an estrogen receptor agonist. Estrogens can increase a normal clear discharge from the vagina and make the vulva and urethra healthy.

PHTPP is a selective ERβ antagonist.

WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER). It acts by inhibiting NF-kB transcriptional activity but being devoid of conventional estrogenic activity.

GLL 398 is an orally active and selective degrader of estrogen receptor with an IC50 of 1.14 nM. GLL 398 blocks tumor growth in xenograft breast cancer models.

Raloxifene (LY-139481) is a selective oestrogen receptor modulator. It has effects on bone and breast cancer and cardiovascular disease risk.

Promestriene (3-propyl ethyl) (INN) is a synthetic estrogen and glucocorticoid used topically in a 1% cream formulation. It is described as a tropic agent and antiseborrheic.

Gestrinone (R 2323) is a synthetic androgen receptor agonist and ER and progesterone receptor antagonist used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.