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.

CBR-470-1 (0.01-10 μM; 24 h) has an EC 50 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 .

2416095-06-0

C14H20ClNO4S2

365.9

CBR-470-1

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years