Catalog No.
Product Name
Application
Product Information
Citations
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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
- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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estrogen ligand
Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER. -
Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
ERRβ agonist
WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM. - (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
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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. -
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). -
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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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. -
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. -
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. -
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. -
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. -
ERα Antagonist
ERα antagonist 1 is a selective covalent antagonist of estrogen receptor α (ERα). It has demonstrated the ability to induce apoptosis and arrest the cell cycle in the G0/G1 phase in MCF-7 breast cancer cells. This compound is valuable for research focused on understanding estrogen signaling pathways and the development of targeted therapies for ERα-positive tumors. -
ERα Degrader
OBHSA is a selective estrogen receptor alpha (ERα) degrader that facilitates the degradation of cyclin D1, effectively bypassing resistance to Tamoxifen. By inducing an increase in intracellular reactive oxygen species, OBHSA activates the unfolded protein response (UPR) excessively, leading to apoptosis in susceptible cells. Additionally, OBHSA serves as an ERα ligand for the synthesis of PROTAC degraders, making it a valuable tool in the study of ERα-mediated pathways and therapeutic resistance in cancer research. -
ER Modulator
MPP hydrochloride is a potent selective modulator of the estrogen receptor (ER). It has been shown to induce significant apoptosis in endometrial cancer and oLE cell lines while antagonizing the positive effects of beta-estradiol. In vivo studies reveal its mixed agonist/antagonist activity on murine uterine ERalpha, making it a valuable tool for research into estrogen-related pathways and cancer therapeutics. -
ERα/ERβ AModulator
Ferutinin, a natural terpenoid compound, modulates estrogen receptors ERα and ERβ, acting as an agonist with an IC50 of 33.1 nM for ERα and exhibiting antagonist properties with an IC50 of 180.5 nM for ERβ. This compound enhances calcium permeability in lipid bilayer membranes and mitochondria, functioning as an electrogenic Ca2+-ionophore. Ferutinin displays a range of biological activities including estrogenic, antitumor, antibacterial, and anti-inflammatory effects, making it a valuable tool for research in cancer biology, hormonal regulation, and inflammation pathways. -
PROTAC ERα Degrader
PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies. -
Estrogen Receptor Modulator
Droloxifene is a selective estrogen receptor modulator (SERM) derived from Tamoxifen. It exhibits antiestrogenic and anti-implantation properties, making it relevant for research in reproductive health. In cellular studies, Droloxifene has been shown to induce p53 expression and promote apoptosis in MCF-7 breast cancer cells. Additionally, it demonstrates protective effects against bone loss in ovariectomized rat models, highlighting its potential applications in osteoporosis research. -
ERα Inhibitor
Isocurcumenol is an estrogen receptor alpha (ERα) inhibitor derived from the rhizomes of Curcuma zedoaria. It demonstrates significant anti-tumor activity, exhibiting IC50 values of 99.1 μg/mL in Dalton's lymphoma ascites (DLA) cells and 178.2 μg/mL in KB cells. This compound has potential applications in cancer research, particularly in exploring targeted therapies for hormone-dependent tumors. -
ERα Degrader
ERα degrader 14 is a selective degrader of estrogen receptor alpha (ERα), primarily functioning through targeted proteasomal degradation. This compound demonstrates potent anti-proliferative effects in ERα-positive breast cancer cell lines, including MCF-7 and T47D, by inducing cell cycle arrest, inhibiting cell migration, and promoting apoptosis. Additionally, ERα degrader 14 effectively suppresses tumor growth in in vivo mouse models, making it a valuable tool for research in breast cancer biology and therapeutic development. -
Estrogen Receptor Modulator
rel-Levormeloxifene is a selective estrogen receptor modulator (SERM) that primarily targets estrogen receptors. This compound effectively inhibits the proliferation of leukemia cells, demonstrating an IC50 of approximately 7 μM. Additionally, rel-Levormeloxifene induces cell cycle arrest at the G0/G1 phase and promotes apoptosis. It also facilitates myelogenesis differentiation while enhancing reactive oxygen species (ROS) production in K562 cells, making it a valuable reagent for research in leukemia and related hematological disorders. -
Estrogen Receptor
BMI-135 is a selective estrogen receptor agonist that mimics estrogen activity. This compound has been shown to induce a rapid endoplasmic reticulum stress response (unfolded protein response, UPR) and promote apoptosis in breast cancer cells. BMI-135 serves as a valuable tool for studying the mechanisms of estrogen signaling and the therapeutic potential of targeting estrogen receptors in breast cancer research. -
Estrogen Receptor Epitope
ERα17p is an epitope derived from the CaM binding site on estrogen receptor alpha (ERα), facilitating its interaction with calmodulin (CaM) in a calcium-dependent manner. This peptide has been shown to regulate the migration of various breast cancer cell lines, including MCF-7, SK-BR-3, T47D, and MDA-MB-231, by activating Rho/ROCK and PI3K/Akt signaling pathways. Additionally, ERα17p exhibits inhibitory effects on breast cancer cell proliferation, induces apoptosis, and suppresses tumor growth in murine models, making it a valuable tool for cancer research. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
ERα Degarder
X15695 is a selective estrogen receptor alpha (ERα) degrader that functions as an aryl hydrocarbon receptor (AHR) ligand. By facilitating the formation of a complex between AHR and ERα, X15695 promotes the proteasomal degradation of ERα, leading to the inhibition of breast cancer cell proliferation. Additionally, it induces cell cycle arrest and apoptosis. This compound is valuable for research in breast cancer biology and therapeutics.
