Catalog No.
Product Name
Application
Product Information
Citations
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ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- Asmaa R. Abdel-Hamed, .et al. , J Med Chem Sci, 2023, 6: 250-268
- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
- Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
- Ewa Domarecka, .et al. , Brain Sci, 2025, Apr 24;15(5):441 PMID: 40426612
- Shuang Liang, .et al. , Cardiovasc Ther, 2022, Apr 7;2022:7145699 PMID: 35474714
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Estrogen receptor agonist
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.- Gao X, .et al. , Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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GPR119 agonist
GSK-1292263 is a novel GPR119 agonist.- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
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Progesterone/ERR Agonist
Etonogestrel is a steroidal progestin used in hormonal contraceptives, most notably the subdermal implant Nexplanon and the vaginal ring NuvaRing.- Linying Li, .et al. , Pharmaceuticals (Basel), 2022, Oct 3;15(10):1226 PMID: 36297338
- Linying Li, .et al. , J Control Release, 2021, Dec 10;340:188-199 PMID: 34678316
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Estrogen receptor antagonist
Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.- Marina Arino Martin, .et al. , Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. , Water Res, 2019, Dec 29;171:115451 PMID: 31901682
- Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
- Muthulakshmi S, .et al. , J Appl Toxicol, 2018, Nov;38(11):1388-1397 PMID: 29923290
- Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene acetate significantly prevents bone mass loss at 20 mg/day in healthy postmenopausal women with normal or low bone mineral density.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
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Estrogen receptor antagonist
Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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ERRβ & ERRγ Agonist
GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.- Shike Zhang, .et al. , Journal of Environmental Sciences, 2024, Oct, 8 PMID: 40412923
- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
- Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
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estrogen receptor modulator
acolbifene is a substance being studied in the prevention of breast cancer in women at high risk of breast cancer. Acolbifene hydrochloride binds to estrogen receptors in the body and blocks the effects of estrogen in the breast. It is a type of selective estrogen receptor modulator (SERM).- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
- Lirit N. Franks, .et al. , Front Pharmacol, 2016, 7: 503 PMID: 28066250
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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Estrogen receptor antagonist
(E/Z)-4-hydroxy Tamoxifen 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.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
- Clomifene inhibits estrogen receptors in hypothalamus, inhibiting negative feedback of estrogen on gonadotropin release, leading to up-regulation of the hypothalamic-Cpituitary-Cadrenal axis.
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ERβ agonist
LY500307 is a potent, selective estrogen receptor beta agonist with an EC50 of 0.66 nM. -
estrogen-receptor modulator
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 ?M and 2.6 ?M, respectively. -
estrogen receptor antagonist
Fulvestrant R enantiomer (ICI 182780 R enantiomer; ZD 9238 R enantiomer; ZM 182780 R enantiomer) is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM. -
estrogen receptor modulators
Pipendoxifene hydrochloride is a selective estrogen receptor modulators (SERMs). -
estrogen receptor covalent antagonist
H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA). -
estrogen receptor (ERα) antagonist
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD). -
oestrogen receptor antagonist
Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property. -
estrogen receptor (ER) inhibitor
WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER) that acts by inhibiting NF-kB transcriptional activity. -
antiestrogenic properties
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus. -
ERRα agonist
Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist. -
Estrogen receptor degrader
SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD). -
estrogen receptor modulator
4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM). -
ERbeta agonist
Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta. -
estrogen receptor degrader
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases. -
PROTAC ERRα Degrader
PROTAC ERRα Degrader-3 is a selective degrader targeting estrogen-related receptor alpha (ERRα) through a von Hippel-Lindau-based mechanism. This compound effectively induces the degradation of ERRα protein by over 80% at a concentration of 30 nM, while showing no activity against ERRβ and ERRγ. It serves as a valuable tool for researchers investigating the role of ERRα in various biological processes and disease states. -
Human Endogenous Metabolite
Estradiol (β-Estradiol) is a steroid hormone and the major female sex hormone. Estradiol can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering. -
PROTAC ERα Degrader
PROTAC ERα Degrader-1 is a bifunctional molecule composed of an estrogen receptor-alpha (ERα) ligand, a linker, and an E3 ubiquitin ligase-recruiting moiety. Derived from compound P1 in patent WO2017201449A1, it functions as a targeted protein degrader that promotes ubiquitination and subsequent proteasomal degradation of ERα. PROTAC ERα Degrader-1 represents a novel approach for modulating estrogen receptor signaling in hormone-dependent cancers. -
estrogen receptor PROTAC protein degrader
Vepdegestrant (ARV-471) is an orally bioavailable PROTAC designed to target and degrade the estrogen receptor (ER). It is being developed for the treatment of patients with locally advanced or metastatic ER+/HER2− breast cancer, offering a novel approach to overcome endocrine resistance through targeted ER degradation. -
Estrogen receptor agonist
4,4'-Sulfonyldiphenol, an estrogen receptor agonist, is a significant chemical interest due to its role as a substitute for Bisphenol A in various industrial and consumer applications. This compound exhibits competitive binding to thyroid hormone receptors with IC50 values of 2650 μM for TRα and 2294 μM for TRβ, influencing breast development and androgen receptor downregulation in fetal testes. Additionally, 4,4'-Sulfonyldiphenol promotes glioblastoma progression by activating the EZH2-mediated PI3K/AKT/mTOR pathway. Chronic exposure can lead to lipid accumulation and metabolic alterations, including dyslipidemia and obesity, while also inducing intestinal inflammation through microbiome disruption and accelerating atherosclerosis in zebrafish models. -
ERα PRRTAC Degrader
GNE-5472 is a potent bifunctional degrader targeting estrogen receptor alpha (ERα) through the PRRTAC mechanism. By functioning as a pan-IAP antagonist, GNE-5472 inhibits cIAP1/2, thereby activating the non-classical NF-κB pathway, which leads to significant upregulation of TNFα expression. This compound effectively inhibits the proliferation of breast cancer cells and promotes apoptosis. GNE-5472 is valuable for research applications in the study of breast cancer and related signaling pathways. -
EGFR Inhibitor, Estrogen Receptor Inhibitor, Progesterone Receptor Inhibitor
4,7-Dihydroxycoumarin is a potent inhibitor of the epidermal growth factor receptor (EGFR) as well as estrogen and progesterone receptors. It exhibits significant cytotoxicity against breast cancer cells, with an IC50 value of 18.36 μg/mL. This compound is valuable for research focused on breast cancer treatment and the exploration of hormone receptor interactions. -
SLU-PP-332 is a pan-Estrogen Receptor/ERR agonist with EC50 values of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, respectively. SLUPP-332 enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. SLU-PP-332 has the potential to study metabolic diseases as well as improve muscle function.
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HDAC
Estrogen Receptor β/HDAC Probe 1 is a near-infrared fluorescent probe designed to simultaneously target the estrogen receptor β and histone deacetylase (HDAC). This probe enables the study of dynamic interactions between these two critical proteins, facilitating the investigation of their roles in cellular signaling and gene regulation. It is particularly useful in cancer research and other studies involving estrogen signaling pathways and epigenetic modifications. -
Estrogen Receptor/ERR Inhibitor
Estradiol cypionate is a 17β-cypionate ester of estradiol that acts as a selective estrogen receptor modulator. It functions by inhibiting the synthesis of endothelin-1 (ET-1), a key factor in vascular biology. This compound is widely utilized in research exploring estrogenic effects, hormonal signaling pathways, and the therapeutic potential of estrogen receptor modulation in various physiological and pathological conditions.
