Home Endocrinology & Hormones Estrogen/progestogen Receptor

Estrogen/progestogen Receptor Modulators

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Signal Transduct Target Ther, 2025, 10(1):97
Cell Death Differ, 2025, 10.1038/s41418-025-01514-7
Cell Rep, 2025, 44(5):115652
Verified customer review of 4-Hydroxytamoxifen (Afimoxifene)
S1972 Tamoxifen Citrate Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). This compound is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. It induces apoptosis and autophagy.
bioRxiv, 2025, 2025.07.21.666025
bioRxiv, 2024, 2023.05.10.540211
EMBO Rep, 2023, 24(5):e55835
Verified customer review of Tamoxifen Citrate
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
Verified customer review of Kaempferol
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
Verified customer review of Bazedoxifene (WAY-140424) HCl
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
Verified customer review of Raloxifene HCl
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
Verified customer review of Clomifene citrate
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
Verified customer review of Toremifene Citrate (NK 622)
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
Verified customer review of Bazedoxifene acetate
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
S8956 (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.
Mol Syst Biol, 2025, 10.1038/s44320-025-00104-6
Oncogene, 2025, 10.1038/s41388-025-03367-3
bioRxiv, 2025, 2024.12.19.629395
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
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
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
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
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
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
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.
S6927 Dihydroresveratrol Dihydroresveratrol is a natural product possessing significant biological activities. This compound, a potent phytoestrogen, is a hormone receptor modulator.
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.
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.
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 .
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.
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.
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.
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.