Estrogen/progestogen Receptor Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2314	Kaempferol	Kaempferol, 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.	BMC Pharmacol Toxicol, 2025, 26(1):167 Int J Mol Sci, 2023, 24(19)14519 Front Pharmacol, 2023, 14:1047184
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.	Cell Death Dis, 2024, 15(4):255 iScience, 2024, 27(10):110862 Int J Mol Sci, 2023, 24(4)3356
S1705	Progesterone	Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. This compound is 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.	Bone Res, 2025, 13(1):37 Cell Proliferation, 2025, e70025 Nat Commun, 2024, 15(1):8708
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.	Viruses, 2024, 16(8)1332 J Pers Med, 2022, 12(2)258 Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2561	Clomifene citrate	Clomifene citrate (NSC 35770, Clomiphene citrate) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.	Biochem Pharmacol, 2024, 232:116694 J Biol Chem, 2024, 300(12):107929 J Pers Med, 2022, 12(2)258
S1859	Diethylstilbestrol	Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.This compound can be used to induce animal models of Pituitary Adenoma.	Communications Medicine, 2025, 1-15 Biomaterials Research, 2024, 0010 iScience, 2024, 27(10):110862
S4154	Cholesterol	Cholesterol(Cholesterin) is the principal sterol of all higher animals required to build and maintain membranes.	Advanced Science, 2025, e2413103 Nat Commun, 2024, 15(1):6740 Nature Communications, 2024, 6740
S1304	Megestrol Acetate	Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.	Scientific Reports, October 06, 2017, 12754 OncoTargets and Therapy, October 03, 2017, 4809-4819 iScience, 2024, 27(10):110862
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.	Viruses, 2024, 16(4)640 Endocrinology, 2021, 162(10)bqab142 bioRxiv, 2020, 2020/9/20.4.7.30734
S8686	PHTPP	PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.	Journal of Agricultural and Food Chemistry, November 28, 2024, 28390-28399 Poultry Science, April 05, 2024, 103734 Biol Pharm Bull, 2025, 48(5):657-671
S6651	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.	Biol Pharm Bull, 2025, 48(5):657-671 iScience, 2024, 27(3):109125 Nutrients, 2023, 16(1)38
S2167	Bazedoxifene acetate	Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM).	Viruses, 2024, 16(8)1332 Journal of Medical Virology, 2022, 4809-4819 Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
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.	Pharmaceutics, 2024, 16(8)1030 Pharmaceutics, 2024, 1030 Biomaterials, 2023, 301:122260
S7828	Licochalcone A	Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.	European Journal of Pharmacology, October 15, 2023, 176031 BioMed Research International, March 10, 2022, 5687832 Oncology Reports, December 14, 2017, 1181-1190
S7839	Endoxifen HCl	Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.	Journal of Molecular Cell Biology, September 11, 2021, 433-444 ACS Omega, October 11, 2021, 27654-27667 Viruses, 2024, 16(8)1332
S3149	Estradiol valerate	Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.	Frontiers in Immunology, October 20, 2022, 1026214 Cell Discovery, August 12, 2025, 68 Cell Discovery, 2025, 68
S1914	Pregnenolone	Pregnenolone(3β-Hydroxy-5-pregnen-20-one) is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.	Cells, 2024, 13(19)1622 Biol Proced Online, 2023, 25(1):31 Communications Biology, 2023, 1026
S4046	Estradiol Cypionate	Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.	Nat Commun, 2024, 15(1):4549 Nature Communications, 2024, 4549 Cell Death Dis, 2024, 15(8):590
S2281	Chrysin	Chrysin (NSC 407436) is a naturally occurring flavone chemically extracted from the blue passion flower (Passiflora caerulea).	Microb Pathog, 2025, 208:107957 Cell Metab, 2022, 34(2):299-316.e6 Cell Metabolism, 2022, 299-316.e6
S1727	Levonorgestrel	Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.	Cancers (Basel), 2025, 17(4)598 Pharmaceuticals -Basel, 2022, 15-101226 J Control Release, 2021, S0168-3659(21)00550-2
S1377	Drospirenone	Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone.	Acta Pharmaceutica Sinica B, 2023, 662-677 Acta Pharm Sin B, 2023, 13(2):662-677 Nature Cancer, 2020, 235-248
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.	J Pain Res, 2025, 18:3573-3592 Neural Plast, 2023, 2023:5225952 Front Pharmacol, 2022, 13:841941
E6030	Bazedoxifene	Bazedoxifene (TSE-424) is a selective estrogen receptor modulator that binds to and activates ERα and ERβ with IC50 values of 26 nM and 99 nM, respectively. It also inhibits IL-6/GP130 interactions, suppresses STAT3 signaling, induces apoptosis, and reduces tumor growth, viability, and colony formation in cancer models, while being studied for effects on bone density, uterine health, and CNS vasomotor responses.	PLOS One, March 24, 2016, e0151182 International Journal of Molecular Sciences, February 08, 2023, 3356 EMBO Molecular Medicine, 2019 Apr, e9539
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 Research, August 14, 2023, 96 Breast Cancer Research and Treatment, April 2020, 635-646 ACS Omega, 2025, 10(15):15256-15271
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.	Journal of Medical Virology, October 2022, 4809-4819 ACS Pharmacology & Translational Science, 2025, nan bioRxiv, 2024 Sep 26, 2024.09.26.615160
S0851	G-1 (LNS 8801)	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.	iScience, 2024, 109125 iScience, 2024, 27(3):109125 Poultry Science, 2024, 103734
S2473	Hexestrol	Hexestrol (Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.	Cell Syst, 2024, 15(12):1107-1122.e7 iScience, 2024, 27(10):110862 Cancers (Basel), 2019 Oct 19, 1596
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.	Nature, 2025, 10.1038/s41586-025-09684-7 The Journal of Clinical Endocrinology & Metabolism, 2019, 6256–6264 J Clin Endocrinol Metab, 2019, 104(12):6256-6264
S1625	Ethinyl Estradiol	Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.	Journal of Cancer, 2021, 4623-4631 Hum Mol Genet, 2020, ddaa244 Regul Toxicol Pharmacol, 2020, S0273-2300(20)30246-4
S8746	H3B-5942	H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values of this compound are 1 nM and 0.41 nM, respectively.	Biol Pharm Bull, 2025, 48(5):657-671 Biological and Pharmaceutical Bulletin, 2025, 657-671 Nat Commun, 2024, 15(1):10170
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.	Chin Med, 2024, 19(1):12 Biomedicine & Pharmacotherapy, 2021 Nov, 112167 Biomedicine & Pharmacotherapy, 2021, 112167
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.	iScience, 2024, 27(10):110862 Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4 Drug Test Anal, 2020, 10.1002/dta.2917
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.	Animal Cells and Systems, 2025, 28-39 iScience, 2024, 109275 Biomedical Reports, 2016, 87-92
S1665	Estrone	Estrone is an estrogenic hormone.	Communications Medicine, 2025, 420 Mol Cell, 2019, 75(6):1103-1116.e9
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. This compound attenuates cellular growth and promotes apoptotic cell death in breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.	Acta Biomater, 2021, S1742-7061(21)00586-9 ACS Synthetic Biology, 2019, 2710-2717
S1858	Dienestrol	Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.	iScience, 2024, 27(10):110862 Biomater Res, 2024, 28:0010
S8958	Camizestrant (AZD9833)	Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.	Cancer Discovery, 2024, 274-289 Viruses, 2024, 1332 Viruses, 2024, 16(8)1332
S1904	Avobenzone	Avobenzone (Butyl methoxydibenzoylmethane, BF2AVB) is an oil soluble ingredient used in sunscreen products to absorb the full spectrum of UVA rays and a dibenzoylmethane derivative.	ProQuest, 2023, 30000028 Reprod Toxicol, 2018, 81:50-57
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). This compound is 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 Research and Treatment, 2020, 635-646 Breast Cancer Res Treat, 2020, 10.1007/s10549-020-05575-9 Nat Genet, 2019, 51(2):207-216
S5236	β-Estradiol 17-Acetate	β-Estradiol 17-Acetate is a metabolite of estradiol which is an estrogen steroid hormone and the major female sex hormone.	Proceedings of EuroResidue IX: Conference on Residues of Veterinary Drugs in Food, 2022, 45 Cell Death & Disease, 2019, 775 Cell Death Dis, 2019, 10(10):775
S1598	Erteberel (LY500307)	Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, demonstrating 32-fold selectivity against estrogen receptor α. It is currently in Phase 2.	University of North Texas, 2014, Health Science Center at Fort Worth
S2450	Equol	Equol, a metabolite of soybeans, is an important isoflavone in humans, specifically binds to 5α-DHT, and has a modest affinity for recombinant estrogen receptor ERβ. Phase 2.	ACS Chem Biol, 2015, 10.1021/cb5009487
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
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.	Pharmaceuticals (Basel), 2022, 16(1)25
E0361	Enclomiphene Citrate	Enclomiphene citrate is the trans isomer of clomiphene citrate and acts as a non-steroidal estrogen receptor antagonist.	Biochem Pharmacol, 2024, 232:116694
E0940	Propyl pyrazole triol (PPT)	Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist.	Ecotoxicol Environ Saf, 2025, 290:117743
S3635	Medroxyprogesterone	Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.	Theranostics, 2024, 593-607
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.	Nat Commun, 2024, 15(1):8708 Nature Communications, 2024, 8708
S5910	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.	Biomater Res, 2024, 28:0010
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).	Cell Regen, 2025, 14(1):18
S4285	Ospemifene	Ospemifene(FC-1271a) is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.	Journal of Medical Virology, October 2022, 4809-4819 Journal of Medical Virology, 2022, 4809-4819
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.	Nat Genet, 2023, 55(2):187-197
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,WL 70) is a progestogen hormonal contraceptive.
S2125	Mestranol	Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.
S3167	Altrenogest	Altrenogest (A35957, RU2267,R2267) is a progestogen structurally related to veterinary steroid trenbolone.
E0527	Norgestimate	Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity.
S0712	Endoxifen E-isomer	Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen and impurity in Endoxifen Z-isomer drug substance, exhibits antiestrogenic effects.
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. This compound exhibits potential anti-tumor activity.
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.
E1301	Imlunestrant	Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells.
S6927	Dihydroresveratrol	Dihydroresveratrol is a natural product possessing significant biological activities. This compound, a potent phytoestrogen, is a hormone receptor modulator.
E0937	Segesterone acetate	Segesterone acetate (Nestoron, ST-1435) is a synthetic progestin that binds to the progesterone receptor with EC50 of 50.3 nM.
E4845	Ulipristal	Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive.
S6601	(±)-Equol	(±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.
E7039	27-Hydroxycholesterol	27-Hydroxycholesterol is an endogenous selective estrogen receptor modulator (SERM) and a a partial agonist of both LXRα and LXRβ. It exhibits partial agonist activity in breast cancer cells and can be used in research on breast cancer risk associated with obesity and hypercholesterolemia.
S3818	Tectoridin	Tectoridin (Shekanin), an isoflavone isolated from flowers of Pueraria thunbergiana, has several pharmacological effects including anti-cancer, anti-inflammatory, antioxidant, and hepatoprotectivy.
E0532	Menotropin	Menotropin (Human Menopausal Gonadotrophin) is a hormonally active medication for the treatment of fertility disturbances, which are extracted from the urine of postmenopausal women.
S4629	Chlorotrianisene	Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.
E8137	Droloxifene	Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
S5676	Zearalenone	Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).
E1903	SLU-PP-332	SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality.
E7063	Endoxifen (Z-isomer)	Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
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.
S5320	Octinoxate	Octinoxate (Octyl methoxycinnamate, ethylhexyl methoxycinnamate) is a cinnamate ester and common ingredient in sunscreen and other skin care products to minimize DNA photodamage.
S5738	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. This compound (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.
S5785	Norethindrone acetate	Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. This compound is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis.
S4638	Desogestrel	Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
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.
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.
S5219	Allylestrenol	Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.
E7105	Coumestrol	Coumestrol, a phytoestrogen present in soybean products, exhibits cytotoxicity via copper-targeted ROS-mediated p53-dependent mechanism in cancer cells. It also suppresses proliferation of ES2 cells with an IC50 of 50 μM.
S4883	Lynestrenol	Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.
E0707	Nomegestrol Acetate	Nomegestrol Acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
S0143	WAY-200070	WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.
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.
E7121	Elacestrant	Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. This compound also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo.
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.
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.
S8986^New	Giredestrant	Giredestrant (GDC-9545; RG6171) is an efficient and potent selective estrogen receptor degrader and a full antagonist with an IC50 of 0.05 nM in T-47D wild-type cells. It also exhibits anti-proliferative activity.
S9609	Amcenestrant (SAR439859)	Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. It is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.
E5720	Isocurcumenol	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.
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.
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.
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.
E1842	Palazestrant	Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER⁺) breast cancer models.
S3160	Ethynodiol diacetate	Ethynodiol diacetate (8080 CB,Ethynodiol acetate) is one of the first synthetic progestogens used in contraceptive pills.
E4947	Estrone sulfate sodium	Estrone sulfate (Estrone 3-sulfate sodium salt, Premarin), an inactive form of estrogen, serves as a major circulating estrogen in the plasma. It is converted into the active form, estrone (E1), through the action of steroid sulfatase (STS. Estrone sulfate is commonly used in breast cancer research.
S2611	Ethisterone	Ethisterone(17α-Ethynyltestosterone) is a progestogen hormone being considered to treat prostate cancer.
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.
E4621	BHPI	BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer.
S5393	Cyclofenil	Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.
E4848	Toremifene	Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
S2567	Medroxyprogesterone Acetate (MPA)	MPA (Medroxyprogesterone acetate) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.	Cancer Sci, 2025, 10.1111/cas.70081 Cell Prolif, 2024, e13780. J Transl Med, 2024, 22(1):478
S5454	Saikosaponin D	Saikosaponin D, a calcium mobilizing agent (SERCA inhibitor), is a type of Saponin derivative, which is a component extracted from Bupleurum falactum. This compound has anti-cancer activities.	Scientific Reports, 2026, Vol 16, Article number: 1 Theranostics, 2025, 8935-8951 Theranostics, 2025, 15(17):8935-8951
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).
S3879	Kaempferide	Kaempferide (4'-Methylkaempferol, 4'-O-Methylkaempferol, Kaempferol 4'-methyl ether), a natural compound derived from the roots of kaempferia galanga, has a variety of effects including anti-carcinogenic, anti-inflammatory, anti-oxidant, anti-bacterial and anti-viral properties.
E7992	Endoxifen	Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
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.
E2401	SPP-86	SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
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.
S3284	Tracheloside	Tracheloside is a lignan glycoside isolated from seeds of Carthamus tinctorius with anti-estrogenic effects. This compound significantly decreases the activity of alkaline phosphatase (AP) (an estrogen-inducible marker enzyme) with IC50 of 0.31 μg/ml. It promotes keratinocyte proliferation through ERK1/2 stimulation.