Estrogen Receptor/ERR Ligand

Epimedin B (Epmedin B) is a flavonoid active component found in Epimedium, with oral activity, and exhibits anti-osteoporotic and neuroprotective effects. Epimedin B inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and mature osteoclast bone resorption, inhibits the phosphorylation of JNK, p38 MAPK, PI3K, and AKT, activates the AMPK-Nrf2 antioxidant pathway, and reduces cellular and mitochondrial ROS. Epimedin B acts on ESR1 and exerts its effects via GPER. Epimedin B alleviates bone loss and improves bone microstructure in vivo, and in Parkinson's models protects dopaminergic neurons and maintains striatal dopamine levels through anti-apoptotic and anti-endoplasmic reticulum stress effects. Epimedin B can be used for research related to osteoporosis, diabetic osteoporosis, and Parkinson's disease.

Segetalin B, an orally active cyclopentapeptide found in Vaccaria segetalis, possesses estrogen-like activity. Segetalin B promotes mineralization of ovariectomized rat-derived bone marrow mesenchymal stem cells (BMSCs) in vitro and increases the level of osteocalcin, BMP-2, ALP, and SIRT1 activity. Segetalin B is promising for research of post-menopausal osteoporosis (PMOP).

β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer.

Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC₅₀ of 41000 μM.

β-Zearalanol-d₄ is the deuterated-labeled β-Zearalenol (HY-N6741). β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer.

ER ligand-13 is a ERα ligand and can be used for the synthesis of PROTACs, such as ERD-3111 (HY-149480).

ERα ligand 2 is a ligand for the PROTAC target protein ERα, which can be used to synthesis of ERα degraders (PROTACs), such as Vepdegestrant (HY-138642).

14-3-3σ/ERRγ stabilizer-1 (compound 4) is a molecular glue and a 14-3-3σ/ERRγ protein-protein interaction stabilizer. 14-3-3σ/ERRγ stabilizer-1 binds to the 14-3-3σ binding groove and tethers via disulfide bond formation with C180 of the ERRγ pS179 phosphopeptide, thereby stabilizing the 14-3-3σ/ERRγ protein complex.

Diisopropyl phthalate-d₄ (DiPP-d₄) is the deuterium labeled Diisopropyl Phthalate (HY-W011926). Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC₅₀ of 41000 μM.

CHEMBL4224880 is an estrogen receptor-α (ER-α) binder.

ER ligand-7 is the ligand for estrogen receptor, and can be used for synthesis of PROTAC ER Degrader-15 (HY-170332) as ligand for target protein.

β-Zearalenol-¹³C₁₈ is the ¹³C-labeled β-Zearalenol (HY-N6741). β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer.

Artonin U is an artonin. Artonin U can be isolated from Artocarpus species. Artonin U binds to hERα, as measured by docking score and Prime MM-GBSA binding free energy evaluation. Artonin U can be used in breast cancer research.

ER ligand-5 is the ligand for estrogen receptor, that can be used as ligand for target protein for PROTAC synthesis of PROTAC ERα Degrader-10 (HY-170336).

ER ligand-14 is an estrogen receptor (ER) ligand. ER ligand-14 can serve as a ligand for target protein for PROTAC, and can be used to develop and design degradative agents for PROTAC ERβ, such as ERB-2 (HY-180850). ERB-2 displays favorable antiproliferative activity against Osimertinib (HY-15772) resistance NSCLC cells.

ERα ligand 6 is an amino intermediate derived from OBHSA, and also serves as a precursor for the synthesis of ERα-targeted hydrophobic tag degraders, such as the ERα ligand moiety of ERα/RAD51 degrader 1 (HY-187096).

ER ligand-11 is the ligand for ERα and can be used for synthesis of PROTACs, such as PROTAC ERα Degrader-12 (HY-174453).

β-Zearalenol (Standard) is the analytical standard of β-Zearalenol (HY-N6741). This product is intended for research and analytical applications. β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer.

ER ligand-14-PEG3-Boc is a conjugate of a target protein ligand and linker, composed of an estrogen receptor ligand and a corresponding linker. ER ligand-14-PEG3-Boc can be used to synthesize PROTACs such as ERB-2 (HY-180850). ERB-2 exhibits good antiproliferative activity against Osimertinib (HY-15772)-resistant non-small cell lung cancer.