Catalog No.
Product Name
Application
Product Information
Citations
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ERα agonist
Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist. -
estrogen receptor modulator
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM). -
Estrogen receptor ligand
α-Estradiol is an endogenous estrogen receptor ligand (Ki values are 0.2 and 1.2 nM for ERα and ERβ receptors respectively). - Estropipate is a form of estrogen, an estrogen receptor agonist. It has several uses such as: Alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics, and treatment of prostate cancer and prevention of osteoporosis.
- Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
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selective Estrogen receptor modulator
Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator. -
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.
- PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
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EStrogen receptor (ER) antagonist
GW7604 is an antiestrogen agbent, and is tthe presumed metabolite of GW5638 in breast (MCF-7) and endometrial (ECC-1) cell lines in vitro. -
ERRa degrader
PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader. -
ERRα Degrader
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader. -
ERRα inverse agonist
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM). -
Estrogen modulator
Bazedoxifene is a third generation selective modulator of estrogen receptor. -
Estrogen receptor modulator
Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. -
estrogen agonist
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist. - Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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ER antagonist
Fulvestrant S enantiomer is the S enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer. -
Estrogen receptor degrader
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. -
SERD/SERM
RAD1901 is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. - Liquiritigenin is a plant-derived highly selective estrogen receptor ?? agonist
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Estrogen receptor degrader
Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. -
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 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 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.
