GDC-0927 (SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
Segetalin B, a cyclopentapeptide from Vaccaria segetalis, possesses estrogen-like activity[1][2].
SLU-PP-332 is a pan-Estrogen Receptor/ERR agonist with EC50 values of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, respectively. SLUPP-332 enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. SLU-PP-332 has the potential to study metabolic diseases as well as improve muscle function[1].
ERα ligand 1 is an estrogen ligand, which targets estrogen receptor α (ERα). ERα ligand 1 binds to cIAP1 ligand Bestatin via a linker to form PROTACs[1].
Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.Target: Estrogen Receptor/ERRA recent study shows that estrogen (estrone, estradiol, and estriol) inhibits Alzheimer's disease-associated low-order Aβ oligomer formation, and among them, estriol shows the strongest in vitro activity [1]. In mPTEN+/- mice, estriol treatments resulted in a 187.54% gain in the relative ratio of uterine wet weight to body weight; estriol also increases the ratio to 176.88% in wild-type mice [2]. Estriol treatment (20 mg/kg ip), in vivo, sensitizes Kupffer cells to LPS via mechanisms dependent on an increase in CD14 by elevated portal blood endotoxin caused by increased gut permeability in rats; while one-half of the rats given estriol intraperitoneally 24 hours before an injection of a sublethal dose of LPS (5 mg/kg) died within 24 hours [3].
R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively[1].
Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.
XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.IC50 value:Target: ERRαERRalpha inverse agonist XCT-790 induced cell death in HepG2 hepatocarcinoma and its multi-drug resistance (MDR) sub-line R-HepG2. Using a dye Mitotracker Green which stains mitochondrion independent of mitochondrial membrane potential (DeltaPsi(m)), XCT-790 dose-dependently decreased mitochondrial mass. Intriguingly, XCT-790 increased DeltaPsi(m) upon short term treatment but decreased DeltaPsi(m) upon longer term treatment. XCT-790 synergized with paclitaxel to induce cell death in multi-drug resistance sub-line R-HepG2 [1].XCT790 is a potent and specific inverse agonist of ERRα. XCT790 shows no significant antagonist activity on related nuclear receptors, such as ERR or ERα at concentrations below 10 μM. This also inhibits the constitutive activity of ER (Estrogen Receptor) [2].
Dienestrol is a synthetic, non-steroidal estrogen, is an estrogen receptor agonist, for the treatment of menopausal and postmenopausal symptoms.
Diarylpropionitrile(DPN) is a non-steroidal estrogen receptor β(ER β) selective ligand.IC50 value:Target: ER β ligandin vitro: Pre-treatment with 1-100 nM DPN significantly decreased neuronal cell death by increasing cell viability through a significant attenuation in the reactive oxygen species level, downregulation of pro-apoptotic activated caspase-3 and Bax, and upregulation of anti-apoptotic Bcl-2, thereby mitigating apoptotic morphological alterations. DPN pre-treatment decreased the expression levels of pro-inflammatory cytokines IL-1β and IL-6 through attenuation of Aβ1-42-induced phosphorylation of mitogen-activated protein kinases JNK and p38. In addition, DPN enhanced ERK1/2 and Akt phosphorylation depressed by Aβ1-42 [1]. ERβ was expressed in RAW264.7 cells, and DPN statistically significantly decreased LPS-induced RANTES production in RAW264.7 cells. Small interfering RNA targeting the ERβ gene inhibited the effect of DPN on RANTES production. In addition, DPN inhibited nuclear translocation and phosphorylation of p65 by inhibiting IκB degradation and thus prohibited the activation of nuclear factor κB (NF-κB) [3].in vivo: DPN treatment during EAE did not attenuate demyelination, only partially improved axon conduction, and did not activate the phosphatidylinositol 3-kinase/serine-threonine-specific protein kinase/mammalian target of rapamycin signaling pathway in ERβ CKO mice [2].
4-Propionamidophenol (compound 4a) is an inactive estrogen receptor ligand based on the diphenylamine skeleton[1].
Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs.
Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2 receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities[1].
Estrone is an estrogenic hormone.Target: Estrogen Receptor/ERREstrone (E1) is an estrogenic hormone secreted by the ovary as well as adipose tissue with the chemical name of 3-hydroxyestra-1,3,5(10)-triene-17-one and the chemical formula C18H22O2. Estrone is one of several natural estrogens, which also include estriol and estradiol. Estrone is the least abundant of the three hormones; estradiol is present almost always in the reproductive female body, and estriol is abundant primarily during pregnancy. Estrone is relevant to health and disease states because of its conversion to estrone sulfate, a long-lived derivative. Estrone sulfate acts as a reservoir that can be converted as needed to the more active estradiol. It is the predominant estrogen in postmenopausal women [1, 2].
4-Nonylphenol-D5 (4-n-Nonylphenol-2,3,5,6-d4,OD) is the deuterium labeled 4-Nonylphenol. 4-Nonylphenol, a major degradation product of Nonylphenol ethoxylates (NPEOs), is a persistent organic pollutant with endocrine-disrupting properties and exerts estrogenic activity[1].
CIDD-0149897 is a potent, selective and brain-penetrant ERβ agonist. CIDD-0149897 exert antitumor functions in glioblastoma[1].
Kaempferide is an O-methylated flavonol, a type of chemical compound. It can be found in Kaempferia galanga (aromatic ginger). The enzyme kaempferol 4'-O-methyltransferase uses S-adenosyl-L-methionine and kaempferol to produce S-adenosyl-L-homocysteine and kaempferide. P-glycoproteins.
Estrone sulfate-d4 (sodium) is deuterium labeled Estrone sulfate (sodium). Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities[1][2].
Cholesterol-18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3][4].
Imlunestrant (LY3484356) is an orally active selective estrogen receptor (ER) degrader (SERD). Imlunestrant (LY3484356) could be used in the study for ER+, HER2-advanced breast cancer[1].
3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells[1].
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility[1][2][3].
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). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.IC50 value: 1.6 μM [1]Target: hERG Potassium Channel, Estrogen Receptor/ERREndoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.[2]
Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors. Lindleyin binds to ERα with estrogenic activity[1].
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations[1].
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively[1][2].