CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.

ARE-LUC:962 nM (EC50)

In IMR32 cells, CBR-470-1, when applied for 24 hours at concentrations ranging from 0.01 to 10 μM, demonstrates an EC50 of 962 nM in the ARE-LUC reporter assay[1].Furthermore, CBR-470-1 induces a dose- and time-dependent accumulation of Nrf2 protein in IMR32 cells when administered at concentrations between 0.5 and 20 μM over a period of 1 to 24 hours[1].In SH-SY5Y cells, a 4-hour treatment with CBR-470-1 at 10 μM activates the Nrf2 signaling cascade[2].Moreover, a 2-hour exposure to CBR-470-1 at 10 μM inhibits MPP+-induced oxidative injury in SH-SY5Y neuronal cells[2].