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

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S8686	PHTPP	PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.	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
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
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
S9862	ARV471	ARV471 is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.	Selective
S4629	Chlorotrianisene	Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.	Selective
S8958	Camizestrant (AZD9833)	Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.	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
S6810	Diarylpropionitrile (DPN)	Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β (ERβ) agonist with EC50 of 0.85 nM, 72-fold more selective for ERβ than ERα.	Selective	estrogen receptor β, EC50: 0.85 nM
S1191	Fulvestrant	Fulvestrant 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(β-Estradiol 3-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 is 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 (LNS 8801) 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	ERα, IC50: 240.4 nM; ERβ, IC50: 165.7 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
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
S4046	Estradiol Cypionate	Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.	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
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
S1859	Diethylstilbestrol	Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.	Selective
S1238	Tamoxifen	Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.	Selective
S3149	Estradiol valerate	Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.	Selective
S1665	Estrone	Estrone is an estrogenic hormone.	Selective
S1972	Tamoxifen (ICI 46474) Citrate	Tamoxifen Citrate (Istubal,ICI 46474 Citrate) 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
S7839	Endoxifen HCl	Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.	Selective
S4285	Ospemifene	Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.	Selective
S1625	Ethinyl Estradiol	Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.	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
S2125	Mestranol	Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.	Selective
S2466	Estriol	Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.	Selective
S2561	Clomifene citrate	Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.	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
S5393	Cyclofenil	Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.	Selective
S2167	Bazedoxifene (TSE-424) acetate	Bazedoxifene Acetate (WAY-140424,TSE-424 acetate) is a third generation selective estrogen receptor modulator (SERM).	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