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Nur77 ligand-binding domain

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-173408
    Nur77 agonist-1

    		Nuclear Hormone Receptor 4A/NR4A Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase Cancer
    Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
    Nur77 agonist-1
  • HY-181588
    NR4A agonist-2

    		Nuclear Hormone Receptor 4A/NR4A Neurological Disease Inflammation/Immunology
    NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis .
    NR4A agonist-2
  • HY-183274
    Nur77 modulator 5

    		Nuclear Hormone Receptor 4A/NR4A Apoptosis PARP Cancer
    Nur77 modulator 5 is a Nur77 modulator. Nur77 modulator 5 induces lysosomal dysfunction, impaired autophagic flux, and apoptosis with increased PARP cleavage, TUNEL positivity, and Annexin V/PI staining. Nur77 modulator 5 can be used for the research of gastric cancer .
    Nur77 modulator 5

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