• Estrogen receptor
  • Progesterone receptor
  • ERR

Estrogen receptor Selective Inhibitors | Activators | Agonists | Antagonists | Chemicals | Modulators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S8372 AZD9496 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models. Selective
S3929 Liquiritigenin Liquiritigenin (4',7-Dihydroxyflavanone), the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, selectively binds to ERβ with an IC50 value of 7.5 μM and activates multiple ER regulatory elements and native target genes with Erβ but not ERα. Selective
S8686 PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα. Selective
S4629 Chlorotrianisene Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator. Selective
S2473 Hexestrol Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. Selective ERα, EC50: 0.07 nM; ERβ, EC50: 0.175 nM
S9609 Amcenestrant (SAR439859) Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation. Selective ERα, EC50: 0.2 nM
S8746 H3B-5942 H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively. Selective ERα WT, Ki: 1 nM; ERα (Y537S), Ki: 0.41 nM
S1191 Fulvestrant (ICI-182780) Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity. Selective ER, IC50: 0.94 nM
S9520 Lasofoxifene Tartrate Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM. Selective estrogen receptor, IC50: 1.5 nM
S4110 Estradiol Benzoate Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM. Selective hERα, IC50: 28 nM; mERα, IC50: 2.3 nM
S5781 Raloxifene Raloxifene (Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. Selective ER, IC50: 5.7 nM
S1227 Raloxifene HCl Raloxifene (LY156758, Keoxifene) HCl a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM. Selective ER, IC50: 5.7 nM
S7855 Brilanestrant (GDC-0810) Brilanestrant (GDC-0810, ARN-810) is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors. Selective ERα, IC50: 6.1 nM; ERβ, IC50: 8.8 nM
S0851 G-1 G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. Selective GPR30, Ki: 11 nM
S2128 Bazedoxifene (WAY-140424) HCl Bazedoxifene HCl (WAY-140424, TSE-424) is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively. Selective ERα, IC50: 23 nM; ERβ, IC50: 89 nM
S9629 Elacestrant (RAD1901) Dihydrochloride Elacestrant (RAD1901) Dihydrochloride is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively. Selective ERα, IC50: 48 nM; ERβ, IC50: 870 nM
S5676 Zearalenone Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER). Selective ERβ, IC50: 165.7 nM; ERα, IC50: 240.4 nM
S5464 Psoralidin Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively. Selective ERα, IC50: 1.03 μM; ERβ, IC50: 24.6 μM
S4046 Estradiol Cypionate Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor. Selective
S7839 Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2. Selective
S2561 Clomifene citrate Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction. Selective
S1972 Tamoxifen (ICI 46474) Citrate Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy. Selective
S4285 Ospemifene Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia. Selective
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis. Selective
S4418 Phenol Red sodium salt Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells. Selective
S1625 Ethinyl Estradiol Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Selective
S3149 Estradiol valerate Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. Selective
S6651 G15 (GRB-G15) G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. Selective
S1665 Estrone Estrone is an estrogenic hormone. Selective
S2125 Mestranol Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. Selective
S2450 Equol Equol ,a metabolite of soybeans, is an important isoflavone in humans,specifically binds to 5α-DHT, has a modest affinity for recombinant estrogen receptor ERβ. Phase 2. Selective
S8958 AZD9833 AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity. Selective
S1776 Toremifene Citrate (NK 622) Toremifene Citrate (NK 622, NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer. Selective
S4440 2-Phenylacetamide 2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells. Selective
S2167 Bazedoxifene (TSE-424) acetate Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM). Selective
S1859 Diethylstilbestrol Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications. Selective
S5393 Cyclofenil Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα. Selective
S1709 Estradiol Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway. Selective
S2466 Estriol Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. Selective
S0503 Estrogen receptor modulator 1 Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity. Selective ER, pIC50: 0.46