estrogen-related receptor

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β with a remarkable affinity (K i = 0.44 nM). This compound exhibits an impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

Estrogen Receptor Antagonist 4 is a potent inhibitor of the estrogen receptor (ER), crucial for regulating cell growth, differentiation, and apoptosis. This compound holds promise for cancer research[1].

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signalling systems play an important role in the regulation of cell growth, differentiation and apoptosis, and Estrogen receptor antagonist 4 has shown potential for research into cancer diseases.

Estrogen receptor antagonist 5 is a potent antagonist of the Estrogen receptor. Estrogen receptor (Estrogen receptor) is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. estrogen receptor antagonist 5 has potential for metastatic disease studies.

Estrogen Receptor Antagonist 7 (Compound 13) is a potent antagonist of estrogen receptors (ER), demonstrating antiproliferative effects against breast and ovarian cancer cells, along with anticancer and anti-uterotrophic activities [1].

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

Estrogen receptor antagonist 2 is a selective down-regulator of estrogen receptor. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. estrogen receptor antagonist 2 has research potential for breast cancer disease.

Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].

Estrogen receptor α antagonist 1 (compound 35) is a highly selective estrogen receptor α antagonist that acts on estrogen receptor α (IC50: 0.02 μM), estrogen receptor β (IC50. Estrogen receptor α antagonist 1 (compound 35) can be used to study tumours.

Estrogen receptor antagonist 1 is a potent antagonist of the estrogen receptor. Estrogen receptor antagonist 1 has shown research potential in breast cancer disease.

Estrogen receptor-IN-1 (compound 16) is an effective estrogen receptor (ER) inhibitor with IC 50 s of 13, 5μM for ERα and Erβ, respectively [1].

Estrogen receptor β antagonist 2 is a selective, potent estrogen receptor β (ERβ) antagonist that acts on Erα (IC50: 109.10 μM) and Erβ (IC50: 0.63 μM).

Estrogen receptor antagonist 6 is a potent antagonist of the Estrogen receptor. Estrogen receptor is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. Compound 166).

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.

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.

Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.

SR 19881 is a full agonist of ERRγ(EC50 value of 0.39 μM in a binding assay and an EC50 value of 4.7 μM in a cell-based assay).

GDC-0927 Racemate is a degrader of estrogen receptor, is used in the research of ER-related diseases, potently inhibits ER-α activity, with an IC50 of 0.2 nM.

(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1, which is an estrogen-related receptor alpha (ERRa) degrader. PROTAC ERRα Degrader-1 consists of an MDM2 ligand binding moiety, a linker and an ERRa binding moiety [1].

(E/Z)-GSK5182 (GSK5182(Z/E)) is a racemic mixture comprising (E)-GSK5182 and (Z)-GSK5182 isomers. It acts as a highly selective and orally active inverse agonist for the estrogen-related receptor γ (ERRγ), demonstrating potency with an IC50 of 79 nM. Additionally, GSK5182 is known to induce the generation of reactive oxygen species (ROS) in hepatocellular carcinoma.

SLU-PP-332 is a pan-estrogen receptor-related receptor (ERR) agonist with high affinity for ERRα, ERRβ, and ERRγ with EC50 values of 98, 230, and 430 nM, respectively.SLUPP-332 enhances mitochondrial function and cellular respiration, increases type IIa oxidized skeletal muscle fibers, and enhances exercise tolerance in skeletal muscle cell lines. SLU-PP-332 has the potential to be used in the study of metabolic diseases and improvement of muscle function, and may be used to ameliorate metabolic disorders and aging.

DK3 is a potent and selective agonist of estrogen-related receptor alpha (ERRα). ERRα is a potential drug target for cancer and metabolic diseases [1].

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

XCT790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα).

DS20362725 is an agonist of estrogen-related receptor α (ERRα) that is able to be used for the metabolic disorders research, for example, type 2 diabetes mellitus (T2DM). The IC 50 value of DS20362725 inhibiting the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) is 0.6 μM [1].

PROTAC ERRα ligand 1 is an α (ERRα) antagonist of estrogen-related receptor (IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively).

PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].

(S,R,S)-AHPC-C5-NH2, also known as VH032-C5-NH2, is a synthetic compound designed as an E3 ligase ligand-linker conjugate. This compound combines the VH032-based von Hippel-Lindau (VHL) ligand with a linker, enabling it to function as a PROTAC degrader for estrogen-related receptor α (ERRα).

Martynoside is a natural selective estrogen receptor modulator, which has antioxidative, anti-muscle fatigue, anticancer and antimetastatic activities. Martynoside has the potential of antagonizing sports anaemia, the mechanism of this effect might be rel

PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist( IC50 : 5.67 nM)

ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist (IC 50=40 nM) [1].

ERRα antagonist-2 (Compound 11) is a potential Reverse agonist of ERR α (estrogen receptor related receptor α) (IC50=0.80 μ M). ERRα antagonist-2 can inhibit the migration and invasion of ER-negative MDA-MB-231 cells. ERRα antiagonist-2 inhibits the growth of breast cancer in vivo.

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM).

(1S,3R)-GNE-502 (compound 179) is a potent degradation agent of Erα and is able to degrade ERα in MCF7 HCS cells (EC50: 13 nM). (1S,3R)-GNE-502 can be used in the study of estrogen receptor-related cancers.

DK1 is a potent estrogen related receptor modulator. DK1 impacts the activity of ERRα receptor and reduces blood glucose. DK1 shows the potential in the diabetes research [1].

(S,R,S)-AHPC-C7-amine, also known as VH032-C7-amine, is a chemically synthesized conjugate that functions as an E3 ligase ligand-linker. This compound combines the VH032-based VHL ligand with a specific linker designed for the degradation of estrogen-related receptor α (ERRα) PROTAC.