erβ

ER-50891 is a potent retinoic acid receptor alpha (RARα) antagonist. er-50891 reduces the inhibitory effect of allosteric retinoic acid and restores osteoblast differentiation induced by bone morphogenetic protein 2.

ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor, exhibits potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model.

ER Proteostasis Regulator-1 (Compound 481) is a potent modulator of endoplasmic reticulum proteostasis with research applications in Alzheimer's disease and diabetes [1].

ER degrader 7 (Compound 35t) is a selective degrader of both ERα and ERβ, and possesses activity as a tubulin polymerization inhibitor. It exhibits potent cell viability inhibition, with IC50 values of 0.06 μM for MCF-7, 2.56 μM for T47D, 15.84 μM for MCF-10A, 1.59 μM for LCC2, 1.67 μM for T47D D538G, and 1.37 μM for T47D Y537S cells. Additionally, ER degrader 7 demonstrates efficacy in suppressing breast cancer tumor growth [1].

ER degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (SERM) with the capacity to degrade Estrogen Receptor (ER)α. It disrupts the microtubule network, inhibiting tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [1].

ER degrader 1 is a potent degrader of the estrogen receptor (ER). The estrogen signaling system plays an important role in the regulation of cell growth, differentiation and apoptosis, and ER degrader 1 has shown potential for cancer diseases.

ER 50891 quarterhydrate is a potent RARα (retinoic acid receptor α) antagonist that markedly diminishes the inhibitory effects of ATRA (all-trans retinoic acid) on osteoblastogenesis induced by BMP 2 (bone morphogenetic protein 2) [1].

ER degrader 3, a potent estrogen receptor (ER) degrader, significantly impacts the estrogen signaling pathway, which is crucial for regulating cell growth, differentiation, and apoptosis. This compound holds potential for cancer research[1].

PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research.

ER-000444793 is a potent mitochondrial permeability transition pore (mPTP) opening inhibitor and it also inhibits mPTP (IC50: 2.8 μM).

ER-27319, an acridone derivative, serves as a potent and selective inhibitor of spleen tyrosine kinase (SYK), effectively impeding both the tyrosine phosphorylation and enzymatic activity of SYK. With an inhibitory concentration (IC50) of 10 µM, this compound suppresses the release of allergic mediators from human and rat mast cells triggered by antigens, making it useful for allergy research [1] [2].

ER Degrader 2, a potent estrogen receptor (ER) degrader, plays a significant role in the estrogen signaling system, which is crucial for regulating cell growth, differentiation, and apoptosis. It holds promise for research in cancer diseases[1].

ER Degrader 5 is a potent compound that degrades the estrogen receptor (ER), exhibits anti-proliferation activity, and has potential applications in breast cancer research [1].

ER-38925 is a retinoic acid receptor (rar) subtype α-selective agonist

ER degrader 4, a selective and orally active compound, effectively degrades estrogen receptors and exhibits anti-tumor activity [1].

LSD1/ER-IN-1 (compound 11g) is a potent inhibitor of ER and LSD1 that acts on LSD1 (IC50: 1.55 μM). LSD1/ER-IN-1 showed good anti-proliferative effect on MCF-7 breast cancer cells (IC50: 8.79 μM).

ER-805751 is a potent proteasome inhibitor.

ER-67880 is a novel and potent microtubule inhibitor with potential anticancer activity.

ER176 is a novel PET radioligand utilized for the visualization of 18 kDa translocator protein (TSPO), a neuroinflammation biomarker, marking the advancement in imaging technology.

SNIPER(ER)-87 is a chemical compound composed of a derivative of the inhibitor of apoptosis protein (IAP) ligand LCL161 conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen using a PEG linker. It effectively degrades the ERα protein with an IC50 value of 0.097 μM. Within cells, SNIPER(ER)-87 selectively recruits XIAP to ERα, and XIAP functions as the primary E3 ubiquitin ligase responsible for the degradation of ERα induced by SNIPER(ER)-87[1][2].

ER-thermo-Yellow is the first fluorescent probe for targeted visualization of temperature at the endoplasmic reticulum with the highest sensitivity reported so far (3.9%/°C).

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, inhibits ERα, and has an EC50 value for estrogen receptor degradation of 0.3 nM.ERα degrader-2 can be used for the prevention and treatment of HER-positive breast cancer.

PROTAC ER Degrader-4 is a PROATC degrader of estrogen receptor (ER)(IC50 of 0.8 nM).

ER272 is a natural PKC activator, inducing hippocampal neurogenesis.

Selective inhibitor of Syk kinase

ERα antagonist 1 is a selective, potent, covalent estrogen receptor alpha (ERα) antagonist that blocks the cell cycle of MCF-7 cells in G0/G1 phase and induces apoptosis.

ERα degrader 6 (Compound 31q) is an ERα degrader with a K I of 75 nM and also inhibits ARO with an IC50 value of 37.7 nM. It effectively inhibits tumor growth in the MCF-7 tumor xenograft model and has applications in breast cancer research [1].

Compound 181, also known as 14-3-3σ/ERα Stabilizer-1, is a covalent stabilizer targeting the 14-3-3σ/ERα proteins. It is utilized in research as a molecular glue [1].

PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader [1] .

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

SNIPER(ER)-110 consists of a cIAP1 ligand and an estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively[1].

ERα degrader 5 is an orally active, selective estrogen receptor (ER) reducer that acts on ERα (EC50: 1.1 nM). ERα degrader 5 shows anti-tumour effects in vivo.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively. The selectivity of Y134 for ERα is 121.1 times higher than that for ERβ. Y134 inhibited the proliferation of ER positive human breast cancer cells stimulated by estrogen.

Cyclopenta[c][1]benzopyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aR,4S,9bS)-rel- is an estrogen receptor beta (ERβ) agonist.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

Prinaberel (ERB-041) is an effective and selective ERβ agonist and >200-fold selective for ERβ.

LY88074 is a raloxifene analog in which the basic side chain has been removed. LY88074 is an agonist of ERβ (EC50 = 232 nM).This compound stimulates uterine cell proliferation.

Acolbifene (SCH 57068) is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6 GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

Bavachin (Corylifolin) is a phytoestrogen that activates the estrogen receptors ERα and ERβ.

PHTPP is a selective ERβ antagonist.

CIDD-0149897 is a potent, selective, and brain-penetrant agonist of ERβ that exhibits antitumor activity in glioblastoma [1].