Estrogen/progestogen Receptor

Choose Selective Estrogen/progestogen Receptor Inhibitors

Estrogen/progestogen Receptor Signaling Pathway Map

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Products

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  • Estrogen/progestogen Receptor Agonists (41)
  • Estrogen/progestogen Receptor Modulators (22)
  • New Estrogen/progestogen Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S5910New Alpha-Estradiol Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.
S8372 AZD9496 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Onco Targets Ther, 2017, 10:4809-4819
S9506 Danazol Danazol (WIN-17757, 2,3-Isoxazolethisterone) is a synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins.
S4440New 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.
S5364 DY131 DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
S9207 Gypenoside XVII Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.
E0361New Enclomiphene Citrate

Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.

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.
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.
Mol Cancer Ther, 2022, 21(1):48-57
Biochim Biophys Acta Gen Subj, 2022, 1866(1):130046
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-2961
S2466 Estriol Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Mol Cell, 2019, 75(6):1103-1116.e9
S2606 Mifepristone (RU486) Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Nat Commun, 2021, 12(1):7041
Exp Eye Res, 2021, S0014-4835(21)00331-6
Oncol Rep, 2021, 46(3)202
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.
Steroids, 2021, 177:108935
Cell Biochem Funct, 2020, 38(1):38-46
S7839 Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
J Mol Cell Biol, 2021, mjab018
Bone, 2020, 130:115123
Mol Cell, 2019, 75(6):1103-1116.e9
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.
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Nat Genet, 2019, 51(2):207-216
S8686 PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
Brain Res, 2021, 1768:147580
Ecotoxicol Environ Saf, 2020, 208:111429
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.
S8958 AZD9833 AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
S9609New 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.
S0358 GSK4716 GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.
S0407 XCT790 XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.
S1625 Ethinyl Estradiol Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
Hum Mol Genet, 2020, ddaa244
Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
S1705 Progesterone (NSC 9704) Progesterone (NSC 9704, NSC 64377, Pregn-4-ene-3,20-dione) is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Thorac Cancer, 2020, 10.1111/1759-7714.13528
Mol Cell, 2019, 75(6):1103-1116.e9
EBioMedicine, 2019, 39:540-551
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.
Sci Adv, 2021, 7(43):eabh1022
Cancer Lett, 2021, 513:36-49
J Steroid Biochem Mol Biol, 2021, 209:105826
S1727 Levonorgestrel Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.
J Control Release, 2021, S0168-3659(21)00550-2
Nat Cancer, 2020, 1(2):235-248
S1858 Dienestrol Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.
S1859 Diethylstilbestrol Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2125 Mestranol Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
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.
ACS Chem Biol, 2015, 10.1021/cb5009487
S2473 Hexestrol Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
S2567 Medroxyprogesterone acetate (NSC-26386) Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
Front Oncol, 2021, 11:665832
Research Square, 2020, 10.21203/rs.3.rs-30247/v1
EBioMedicine, 2019, 44:563-573
S2604 Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2
J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002
SSRN, 2021, 10.2139/ssrn.3886996
S2611 Ethisterone Ethisterone is a progestogen hormone being considered to treat prostate cancer.
S3149 Estradiol valerate Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
S3160 Ethynodiol diacetate Ethynodiol diacetate (8080 CB) is one of the first synthetic progestogens used in contraceptive pills.
S3167 Altrenogest Altrenogest (A35957, RU2267) is a progestogen structurally related to veterinary steroid trenbolone.
S3449 GSK5182 GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
S3617 (20S)-Protopanaxatriol (20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).
S3635 Medroxyprogesterone Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.
S3657 Promestriene Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.
S3671 Quinestrol Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.
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.
Mol Med Rep, 2021, 24(4)686
Mol Med Rep, 2021, 24(4)686
S4046 Estradiol Cypionate Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.
Autophagy, 2016, 12(9):1593-613
S4097 Dydrogesterone Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.
S4110 Estradiol Benzoate Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.
Nutr Metab (Lond), 2021, 18(1):63
S4154 Cholesterol Cholesterol is the principal sterol of all higher animals required to build and maintain membranes.
EMBO Rep, 2021, e52537
Graefes Arch Clin Exp Ophthalmol, 2021, 10.1007/s00417-021-05328-4
Nat Commun, 2019, 11;10(1):4621
S4507 17-Hydroxyprogesterone 17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
S4638 Desogestrel Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
S4673 Etonogestrel Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.
S4674 Hydroxyprogesterone caproate Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.
S4883 Lynestrenol Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
S5288 Estropipate Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.
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.
S5469 Bavachin Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.
S5676 Zearalenone Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
S5872 Estradiol dipropionate Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.
S6601 (±)-Equol (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.
S6810New 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.
S7828 Licochalcone A Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
Environ Toxicol, 2021, 10.1002/tox.23422
S9629New 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.
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.
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
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.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
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.
Endocrinology, 2021, 162(10)bqab142
bioRxiv, 2020, 2020/9/20.4.7.30734
J Virol, 2019, 93(8)
S1914 Pregnenolone Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
J Sep Sci, 2019, 42(10):1833-1841
Phytother Res, 2018, 32(6):996-1003
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.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Cell Chem Biol, 2021, S2451-9456(21)00400-1
Transl Oncol, 2021, 14(11):101192
S2167 Bazedoxifene (TSE-424) acetate Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM).
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Transl Oncol, 2021, 14(11):101192
Mol Cancer Ther, 2020, 7 pii: molcanther
S2301 Genistin (Genistoside) Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.
Acta Biomater, 2021, S1742-7061(21)00586-9
S2314 Kaempferol (NSC 407289) Kaempferol (NSC 407289, Robigenin), a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Molecules, 2021, 26(5)1210
Eur J Pharmacol, 2021, 907:174251
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S2561 Clomifene citrate Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S3081 Ulipristal Acetate (CDB 2914) Ulipristal acetate (CDB-2914, HRP 2000, RU 44675) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
J Clin Endocrinol Metab, 2019, 104(12):6256-6264
Cell Prolif, 2017, 50(5)
S4285 Ospemifene Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
S4629 Chlorotrianisene Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
S5393 Cyclofenil Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
S5738New Megestrol Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Drug Test Anal, 2020, 10.1002/dta.2917
S6927New Dihydroresveratrol Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.
S7827 4-Hydroxytamoxifen (Afimoxifene) 4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
Sci Adv, 2021, 7(43):eabh1022
Nat Commun, 2021, 12(1):6020
BMC Cancer, 2021, 21(1):931
S8956New (Z)-4-Hydroxytamoxifen (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.
S9122 Tectorigenin Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.
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.
Mol Cancer Res, 2021, 19(6):1026-1039
S1251 Dienogest Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.
S1376 Gestodene Gestodene (SH B 331) is a progestogen hormonal contraceptive.
S1377 Drospirenone Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone.
Nat Cancer, 2020, 1(2):235-248
J Thromb Haemost, 2015, 13(10):1918-24
S1665 Estrone Estrone is an estrogenic hormone.
Mol Cell, 2019, 75(6):1103-1116.e9
S4418New 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.
S5219New Allylestrenol Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.
S5785New Norethindrone acetate Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. Norethindrone acetate is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis.
S1304 Megestrol Acetate Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S5910New Alpha-Estradiol Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.
S8372 AZD9496 AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Onco Targets Ther, 2017, 10:4809-4819
S9506 Danazol Danazol (WIN-17757, 2,3-Isoxazolethisterone) is a synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins.
S4440New 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.
S5364 DY131 DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
S9207 Gypenoside XVII Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.
E0361New Enclomiphene Citrate

Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.

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.
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.
Mol Cancer Ther, 2022, 21(1):48-57
Biochim Biophys Acta Gen Subj, 2022, 1866(1):130046
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-2961
S2466 Estriol Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Mol Cell, 2019, 75(6):1103-1116.e9
S2606 Mifepristone (RU486) Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Nat Commun, 2021, 12(1):7041
Exp Eye Res, 2021, S0014-4835(21)00331-6
Oncol Rep, 2021, 46(3)202
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.
Steroids, 2021, 177:108935
Cell Biochem Funct, 2020, 38(1):38-46
S7839 Endoxifen HCl Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
J Mol Cell Biol, 2021, mjab018
Bone, 2020, 130:115123
Mol Cell, 2019, 75(6):1103-1116.e9
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.
Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9
Nat Genet, 2019, 51(2):207-216
S8686 PHTPP PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
Brain Res, 2021, 1768:147580
Ecotoxicol Environ Saf, 2020, 208:111429
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.
S8958 AZD9833 AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
S9609New 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.
S0358 GSK4716 GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.
S0407 XCT790 XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.
S1625 Ethinyl Estradiol Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
Hum Mol Genet, 2020, ddaa244
Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
S1705 Progesterone (NSC 9704) Progesterone (NSC 9704, NSC 64377, Pregn-4-ene-3,20-dione) is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Thorac Cancer, 2020, 10.1111/1759-7714.13528
Mol Cell, 2019, 75(6):1103-1116.e9
EBioMedicine, 2019, 39:540-551
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.
Sci Adv, 2021, 7(43):eabh1022
Cancer Lett, 2021, 513:36-49
J Steroid Biochem Mol Biol, 2021, 209:105826
S1727 Levonorgestrel Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.
J Control Release, 2021, S0168-3659(21)00550-2
Nat Cancer, 2020, 1(2):235-248
S1858 Dienestrol Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.
S1859 Diethylstilbestrol Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2125 Mestranol Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
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.
ACS Chem Biol, 2015, 10.1021/cb5009487
S2473 Hexestrol Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
S2567 Medroxyprogesterone acetate (NSC-26386) Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
Front Oncol, 2021, 11:665832
Research Square, 2020, 10.21203/rs.3.rs-30247/v1
EBioMedicine, 2019, 44:563-573
S2604 Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2
J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002
SSRN, 2021, 10.2139/ssrn.3886996
S2611 Ethisterone Ethisterone is a progestogen hormone being considered to treat prostate cancer.
S3149 Estradiol valerate Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
S3160 Ethynodiol diacetate Ethynodiol diacetate (8080 CB) is one of the first synthetic progestogens used in contraceptive pills.
S3167 Altrenogest Altrenogest (A35957, RU2267) is a progestogen structurally related to veterinary steroid trenbolone.
S3449 GSK5182 GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
S3617 (20S)-Protopanaxatriol (20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).
S3635 Medroxyprogesterone Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.
S3657 Promestriene Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.
S3671 Quinestrol Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.
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.
Mol Med Rep, 2021, 24(4)686
Mol Med Rep, 2021, 24(4)686
S4046 Estradiol Cypionate Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.
Autophagy, 2016, 12(9):1593-613
S4097 Dydrogesterone Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.
S4110 Estradiol Benzoate Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.
Nutr Metab (Lond), 2021, 18(1):63
S4154 Cholesterol Cholesterol is the principal sterol of all higher animals required to build and maintain membranes.
EMBO Rep, 2021, e52537
Graefes Arch Clin Exp Ophthalmol, 2021, 10.1007/s00417-021-05328-4
Nat Commun, 2019, 11;10(1):4621
S4507 17-Hydroxyprogesterone 17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
S4638 Desogestrel Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
S4673 Etonogestrel Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.
S4674 Hydroxyprogesterone caproate Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.
S4883 Lynestrenol Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
S5288 Estropipate Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.
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.
S5469 Bavachin Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.
S5676 Zearalenone Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
S5872 Estradiol dipropionate Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.
S6601 (±)-Equol (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.
S6810New 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.
S7828 Licochalcone A Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
Environ Toxicol, 2021, 10.1002/tox.23422
S9629New 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.
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.
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
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.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
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.
Endocrinology, 2021, 162(10)bqab142
bioRxiv, 2020, 2020/9/20.4.7.30734
J Virol, 2019, 93(8)
S1914 Pregnenolone Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.
J Sep Sci, 2019, 42(10):1833-1841
Phytother Res, 2018, 32(6):996-1003
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.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Cell Chem Biol, 2021, S2451-9456(21)00400-1
Transl Oncol, 2021, 14(11):101192
S2167 Bazedoxifene (TSE-424) acetate Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM).
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Transl Oncol, 2021, 14(11):101192
Mol Cancer Ther, 2020, 7 pii: molcanther
S2301 Genistin (Genistoside) Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.
Acta Biomater, 2021, S1742-7061(21)00586-9
S2314 Kaempferol (NSC 407289) Kaempferol (NSC 407289, Robigenin), a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Molecules, 2021, 26(5)1210
Eur J Pharmacol, 2021, 907:174251
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S2561 Clomifene citrate Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S3081 Ulipristal Acetate (CDB 2914) Ulipristal acetate (CDB-2914, HRP 2000, RU 44675) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
J Clin Endocrinol Metab, 2019, 104(12):6256-6264
Cell Prolif, 2017, 50(5)
S4285 Ospemifene Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
S4629 Chlorotrianisene Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
S5393 Cyclofenil Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
S5738New Megestrol Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
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.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Drug Test Anal, 2020, 10.1002/dta.2917
S6927New Dihydroresveratrol Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.
S7827 4-Hydroxytamoxifen (Afimoxifene) 4-Hydroxytamoxifen (Afimoxifene) is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
Sci Adv, 2021, 7(43):eabh1022
Nat Commun, 2021, 12(1):6020
BMC Cancer, 2021, 21(1):931
S8956New (Z)-4-Hydroxytamoxifen (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.
S9122 Tectorigenin Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.
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.
Mol Cancer Res, 2021, 19(6):1026-1039
S5910New Alpha-Estradiol Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.
S4440New 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.
E0361New Enclomiphene Citrate

Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.

S9609New 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.
S6810New 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.
S9629New 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.
S5738New Megestrol Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
S6927New Dihydroresveratrol Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.
S8956New (Z)-4-Hydroxytamoxifen (Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.
S4418New 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.
S5219New Allylestrenol Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.
S5785New Norethindrone acetate Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. Norethindrone acetate is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis.