CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade[1][2].
CBR-470-1 (0.01-10 μM; 24 h) has an EC50 of 962 nM in ARE-LUC reporter assay of IMR32 cells[1].
CBR-470-1 (0.5-20 μM; 1-24 h) results in a dose- and time-dependent accumulation of Nrf2 protein in IMR32 cells[1].
CBR-470-1 (10 μM; 4 h) activates Nrf2 signaling cascade in SH-SY5Y cells[2].
CBR-470-1 (10 μM; 2 h) inhibits MPP+-induced oxidative injury in SH-SY5Y neuronal cells[2].
Western Blot Analysis[1]
| Cell Line: | IMR32 cells |
| Concentration: | 0.5, 1, 5, 10, 20 μM |
| Incubation Time: | 1, 2, 4, 8, 24 h |
| Result: | Increased the Nrf2 protein in a dose- and time-dependent manner. Increased both mRNA and protein levels of the Nrf2-responsive genes NQO1 and HMOX1. |