Estrogen Receptor/ERR

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.

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.

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.

Coumestrol that existed in soybean products suppresses the proliferation of ES2 cells (IC50: 50 μM). It exhibits activities against neurological disorders, cancers and autoimmune diseases.

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.

(E Z)-4-Hydroxytamoxifen (Afimoxifene) is a novel estrogen inhibitor, commonly used in research for various estrogen-dependent conditions, including cyclic mastalgia and gynecomastia.

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.

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

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

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).

Saikosaponin D is a novel SERCA inhibitor by inhibiting NF-κB and STAT3 signaling to protect against acetaminophen-induced hepatotoxicity.

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].

Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .

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

Giredestrant (GDC-9545) potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist.

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.

PHTPP is a selective ERβ antagonist.

(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.

Delphinidin chloride, a natural plant pigment found in berries and red wine, is a precursor of certain anthocyanins. Delphinidin chloride induces the release of nitric oxide from the vascular endothelium, resulting in vascular relaxation. At the dose of 1-40 μM, epithelial growth factor receptor signaling and estrogen receptor α expression were inhibited, which was associated with apoptosis and autophagy. Delphinidin chloride regulates JAK STAT3 and MAPKinase signaling. Delphinidin also inhibited the histone acetyltransferase activity of p300 CBP (IC50 was about 30 μM).

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.

Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

Enclomiphene citrate (trans-Clomiphene citrate) is a non-steroidal estrogen receptor antagonist,with antioestrogenic property

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.

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

Pipendoxifene hydrochloride is a selective modulator of estrogen receptor.

1. Isocurcumenol inhibits 5α-reductase which converts testosterone to dihydrotestosterone (DHT).

Premarin (Estrone 3-sulfate) is an an estrogen sulfate with neuroprotective actions during traumatic brain injury.

(-)-(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.

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

Propyl pyrazole triol (PPT) is a selective agonist of estrogen receptor alpha (ERα), exhibiting a relative binding affinity of 49% for ERα, which is approximately 410 times higher than its affinity for estrogen receptor beta (ERβ: 0.12%).

Diethylstilbestrol (DES) is used in the treatment of menopausal and postmenopausal disorders.

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

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.

Norethindrone acetate (19-Norethindroneacetate) is an oestrogen with inhibitory effects on adolescent menstruation and hepatic adenomas and is often used in combination with progestins in the study of endometriosis.

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

XCT790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα).

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

DY131 (DY-131) is a novel selective agonist of ERRβ and ERRγ.

(20S)-Protopanaxatriol (g-PPT)(g-PPT), a metabolite of ginsenoside, could regulate endothelial cell functions through the estrogen receptor and glucocorticoid receptor.

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

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

α-Zearalenol is one of the major metabolites of Zearalenone. α-Zearalenol has structural analogy to estrogen, thus α-Zearalenol can bind to estrogen receptors (ERs).

MPP hydrochloride is a selective estrogen receptor (ERR) modulator.

Endoxifen E-isomer (E-Endoxifen) is the E-isomer of (Z)-Endoxifen. Endoxifen E-isomer has antiestrogenic effects.

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