ERα Antagonist

OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC₅₀ values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research.

GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.

Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC₅₀ = 2 nM) and ERβ (IC₅₀ = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.

Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (K_i=0.09 nM) over ERβ (K_i=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.

Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC₅₀s of 109.10, 0.63 µM for Erα and Erβ, respectively.

ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells.

ERRα ligand 2 is a ERRα ligand with a target IC₅₀ of 5.67 nM. PROTAC ERRα ligand 2 blocks the protein-protein interaction between ERRα and PGC-1α. PROTAC ERRα ligand 2 can be used for synthesis of PROTACs.

(R,R)-THC is an ERα agonist and an ERβ antagonist, with K_is of 9.0 nM and 3.6 nM for ERα and ERβ, respectively. (R,R)-THC has higher relative binding affinity for ERβ than ERα with the values of 25 and 3.6.

Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC₅₀=2 nM) and ERβ (IC₅₀=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.

ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC₅₀ of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.

ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC₅₀ value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer.

SNG-8023 is an anti-ERα humanized monoclonal antibody. SNG-8023 can be used for cancer research, such as breast cancer.

Mansonone F acts as an estrogen receptor antagonist and an antimicrobial agent. Mansonone F effectively inhibits 17β-estradiol-induced β-galactosidase activity. Derivatives of Mansonone F also exhibit antioxidant and anti-Staphylococcus aureus biological activities. Mansonone F can be used in studies related to Staphylococcus aureus infections and methicillin-resistant Staphylococcus aureus (MRSA) infections.

ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC₅₀ value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer.

ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and ERβ. ERα/ERβ antagonist-1 reduces ERα and ERβ activity in a dose-dependent manner in HepG2 liver cells.