Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM)[1].
GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects[1].
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an >IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM)[1].
G-36 is a cell permeable non-steroidal antagonist of G-protein-coupled estrogen receptor (GPER/GPR30) which selectively inhibits estrogen-mediated activation of PI3K by GPER, but not by ERα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM)[1].
Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6[1].
G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity[1][2].
Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively[1][2].
SLU-PP-915 is an agonist of ERR. SLU-PP-915 has an EC50 value of approximately 400 nM for ERRα, ERRβ, and ERRγ. SLU-PP-915 has potential application in maintaining oxidative metabolism and heart failure[1][2][3].
Cholesterol-d1 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].
Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER),α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects[1].
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively[1].
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively[1].
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender specific neuroprotection in a Parkinson’s Disease rat model[1].
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].
Cholesterol-d6 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].
SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively[1].
Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
PROTAC ER Degrader-4 is a PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM[1].
Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis[1][2].
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A[1].
Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα, due to its additional non-covalent interactions with Y326 and N346 at the active site of ERRγ. GSK5182 also induces Reactive Oxyen Species (ROS) generation in hepatocellular carcinoma (HCC)[1][2][3].
Estrogen receptor antagonist 2 is a potent and orally active estrogen receptor (ER) antagonist, example 17, extracted from patent US20180111931A1. Estrogen receptor antagonist 2 is used for the study of breast cancer[1].
Estropipate is a form of estrogen, used to treat symptoms of menopause, also used to prevent osteoporosis.
(±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogen receptor modulator (SERM) (Estrogen Receptor/ERR) that inhibits ERα and ERβ with IC50s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research[1][2].
Toremifene (NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.IC50 Value: 1±0.3 μMTarget: Estrogen receptorToremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT in men with prostate cancer [1]. in vitro: The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3μM, 1±0.3μM and 60.4±17.2μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro[2].in vivo: The effect of this combination was then studied in vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone[2].Clinical trail: Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene[3].