Z-DEVD-FMK

Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with an IC₅₀ of 18 μM^[1]. IC50 & Target: IC50: 18 μM (caspase-3)^[1] In Vitro: N27 cells are exposed to MPP⁺ in the absence or presence of 50 μM Z-DIPD-FMK or 100 μM Z-DEVD-FMK or 50 μM Z-LEHD-FMK and then caspase-9 and caspase-3 enzymatic activities are determined by enzymatic assay at 12 and 24 h following exposure, respectively. Exposure to 300 μM MPP⁺ for 24 h in N27 cells results in an approximately 2.5-fold increase in caspase-3 enzyme activity. MPP⁺-induced increases in caspase-3 enzyme activity are significantly blocked by 50 μM Z-DIPD-FMK, 100 μM Z-DEVD-FMK, and 50 μM Z-LEHD-FMK^[1]. In Vivo: Early Z-DEVD-FMK (160 ng) treatment improves motor and cognitive function after traumatic CNS injury induced by severe controlled cortical impact (CCI) in the mouse^[2]. Treatment with Z-DEVD-FMK (160 ng) significantly improves neurological outcome when compared with traumatized animals treated with DMSO vehicle (p<0.01)^[3].