Estrogen Receptor/ERR Ligand

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).

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.

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

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.

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.

HGH fragment 176-191 is a fragment of Human Growth Hormone. HGH fragment 176-191 binds with high affinity to Ki-67, MiB proteins, and estrogen receptors. HGH fragment 176-191 enhances the toxicity of chitosan nanoparticles loaded with Doxorubicin (HY-15142A) against breast cancer. HGH fragment 176-191 promotes lipolysis and fat utilization in mice. HGH fragment 176-191 can be used in research related to targeted drug delivery for cancer and lipid metabolism.

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.

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

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.

ER ligand-16 is a PROTAC target protein ligand that binds specifically to Estrogen Receptor, and it is applicable to research related to PROTAC synthesis, such as serving as the target protein ligand for PROTAC ERα Degrader-4 (HY-149295).

AZD9496 deacrylic acid phenol is a fragment of target protein ligand of PROTAC ER Degrader-4 (HY-135309).

ERα ligand 4 is a ligand of ERα and can be used for the synthesis of PROTACs, such as NEP168 (HY-180959).

Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC₅₀ values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes.

ERα ligand 5 (Compound 53) is a ERα ligand that can be used for the synthesis of PROTACs, such as ERD-308 (HY-128600).

HDAC6/ERα ligand-1 is a dual-target ligand with inhibitory activity against both estrogen receptor α (ERα) and histone deacetylase 6 (HDAC6). HDAC6/ERα ligand-1 can be used to synthesize PROTACs, such as PROTAC HDAC6/ERα degrader 1 (HY-187387). HDAC6/ERα ligand-1 binds to the ligand-binding pocket of ERα and forms hydrogen bonds with specific residues in helices 10, 11 and 12. HDAC6/ERα ligand-1 binds stably to HDAC6 and forms hydrogen bonds with specific residues of this protein. HDAC6/ERα ligand-1 can be used in breast cancer research.

ER ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). ER ligand-3 can be used for the synthesis of PROTAC ER Degrader-12 (HY-160264).