estrogen-related receptor

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).

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.

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.

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

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.

ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective, and orally bioavailable estrogen-related receptor gamma (ERRγ) inverse agonist with an IC50 of 40 nM [1].

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.

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

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].

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].

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

(S,R,S)-AHPC-C5-NH2, also known as VH032-C5-NH2, is a synthetic 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).

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

PROTAC ERRα ligand 2 is an inverse agonist for the estrogen-related receptor α (ERRα) with an IC50 of 5.67 nM.

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

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].

DS20362725 is a selective estrogen-related receptor alpha (ERRα) agonist that binds to ERRα and enhances its transcriptional activity while preventing ERRα from binding to its repressor, receptor-interacting protein 140 (RIP140), commonly used in the study of metabolic disorders.

ERRα antagonist-2 (Compound 11) is an estrogen-related receptor α inverse agonist with an IC50 of 0.80 μM, capable of inhibiting migration and invasion in ER-negative MDA-MB-231 cells and suppressing breast cancer growth.

(1S,3R)-GNE-502 (compound 179) is a potent ERα degradation agent with an EC50 of 13 nM in MCF7 HCS cells, suitable for studying estrogen receptor-related cancers.

(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, exhibiting EC50 values of 98, 230, and 430 nM, respectively. SLU-PP-332 enhances mitochondrial function and cellular respiration, increases type IIa oxidized skeletal muscle fibers, and enhances exercise tolerance in skeletal muscle cell lines. It has potential applications in the study of metabolic diseases, improvement of muscle function, and amelioration of metabolic disorders and aging.

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

Pelargonidin-3-O-glucopyranoside is the glucoside of Pelargonidin, an potential antidiabetic agent. Pelargonidin-3-O-glucopyranoside has antioxidant, anti-inflammatory, anti-estrogenic, and angiotensin-converting enzyme inhibitory activities.