Nur77

TMPA is a novel small molecule that binds to orphan Nuclear Receptor Nur77 with high affinity (Kd = 1.45 ?? 0.35 μM), and interferes with the Nur77-LKB1 interaction.

DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. Antineoplastic activity.

DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.

Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.

DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist.

Nur77 agonist-1 is a selective agonist targeting the Nur77 receptor, promoting ferroptosis through the upregulation of Nur77 protein expression. This compound significantly elevates levels of reactive oxygen species (ROS) and lipid peroxidation while diminishing GPX4 protein expression. With a binding affinity of 13.80 μM to the ligand binding domain of Nur77, Nur77 agonist-1 demonstrates potent antiproliferative effects against various breast cancer cell lines (IC50: 2.15-3.26 μM) while exhibiting low toxicity to normal cells. It is a valuable tool for research focused on breast cancer therapies.

Nur77 Modulator 1 is an effective modulator of Nur77, characterized by a binding affinity of KD = 3.58 μM. This compound up-regulates Nur77 expression and influences its sub-cellular localization, leading to Nur77-dependent endoplasmic reticulum (ER) stress and autophagy, ultimately promoting apoptotic processes in cells. Its notable anti-hepatoma activity makes it a valuable tool for research in cancer biology and cellular stress responses.

Nur77 Antagonist 1 is a selective antagonist of the Nur77 receptor, with a binding affinity of KDSPR Nur77 = 91 nM. This compound has demonstrated the ability to induce apoptosis in cancer cells, showcasing significant antitumor activity against triple-negative breast cancer (TNBC) cells. It serves as a valuable tool for research in cancer biology and therapeutic development targeting Nur77 pathways.

Nur77 modulator 3 is an effective modulator of Nur77, targeting the regulation of hepatic stellate cell (HSC) activation. This compound induces Nur77 expression, leading to decreased ECM deposition and enhanced autophagic flux that is dependent on Nur77. Additionally, it significantly inhibits the mTORC1 signaling pathway, resulting in reduced inflammation and amelioration of hepatic fibrosis in vivo. Nur77 modulator 3 is particularly useful for studies related to liver pathology and fibrosis research.

4-PQBH is a potent binder of Nur77, exhibiting a dissociation constant (KD) of 1.17 μM. This compound significantly induces caspase-independent cytoplasmic vacuolization and paraptosis through the mediation of endoplasmic reticulum (ER) stress and autophagy pathways. 4-PQBH serves as a valuable tool for cancer research, particularly in the study of cell death mechanisms and neurodegenerative disorders.