Nrf2 HO-1 activator 2 (compound 13m), a difluoro-substituted derivative, is a highly potent activator of Nrf2 HO-1. It exhibits substantial neuroprotective and antioxidant properties by activating the Nrf2 HO-1 pathway through phosphorylation of ERK1 2, JNK, or Akt in PC12 cells. This compound finds utility in the investigation of Parkinson's disease (PD) [1].
Nrf2 activator-2 (referred to as compound O15), an Osthole derivative, is a highly potent Nrf2 agonist exhibiting an EC 50 of 2.9 μM in 293 T cells. By effectively disrupting the binding between Keap1 and Nrf2, Nrf2 activator-2 activates the Nrf2 pathway. Furthermore, this compound significantly reduces the ubiquitination of Nrf2 in cells, indicating its potential in regulating Nrf2 activity [1].
R079 (compound 17), a selective and orally active Nrf2 activator, enhances Nrf2 translocation activity (EC 50 = 32.41 μM) and can neutralize excess levels of reactive oxygen species by activating Nrf2. Additionally, R079 possesses anti-inflammatory properties and has applications in multiple sclerosis research [1].
Fraxinellone analog 1 (compound 2) 作为一种Nrf2介导的抗氧化防御系统激活剂,显示出高效和迅速的效应,并对谷氨酸诱导的兴奋性毒性提供保护.它通过诱导Gpx4、Sod1和Nqo1等抗氧化基因的表达来发挥作用.此外,Fraxinellone analog 1 还具备神经保护特性,可调节抗氧化应激和炎症,适用于神经退行性疾病的相关研究.