Nurr1 agonist 14 is a selective Nurr1 agonist with an human EC50 0.09 µM and a KD of 0.2 µM. Nurr1 agonist 14 shows weaker activity on Nur77 (EC50 = 0.16 µM) and NOR1 (EC50 = 0.12 µM). Nurr1 agonist 14 activates Nurr1 by diminishing Nurr1 dimer formation to release transcriptionally active Nurr1 monomer. Nurr1 agonist 14 has significant neuroprotective activity with no influence of residual DHODH inhibition. Nurr1 agonist 14 upregulates neuroprotective genes including SOD2, SESN3, BIRC5, XIAP, FLRT2 and CRMP4 in dopaminergic neurons. Nurr1 agonist 14 can be used for neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD) and multiple sclerosis (MS) research[1].
