Definition
ChEBI: Z-DEVD-FMK is a tetrapeptide consisting of Fmoc-L-aspartic acid 4-methyl ester, methyl L-alpha-glutamic acid 5-methyl ester, L-valine and the fluoromethyl ketone derived from the 1-carboxy group of L-aspartic acid 4-methyl ester coupled in sequence. It is a specific, irreversible caspase-3 inhibitor that also shows potent inhibition of caspase-6, caspase-7, caspase-8, and caspase-10. It has a role as an apoptosis inhibitor, an EC 3.4.22.56 (caspase-3) inhibitor and a neuroprotective agent.
General Description
A potent, cell-permeable, and irreversible inhibitor of caspase-3 as well as caspase-6, caspase-7, caspase-8, and caspase-10. When using with purified native or recombinant enzyme, pretreatment with an esterase is required. A 5 mM (250 μg/75 μl) solution of Z-DEVD-FMK (Cat. No.
264156) in DMSO is also available.
References
1. garcia-calvo m, peterson ep, leiting b, ruel r, nicholson dw, thornberry na (1998) inhibition of human caspases by peptidebased and macromolecular inhibitors. j biol chem 273:32608–32613 2. thornberry na, rano ta, peterson ep, rasper dm, timkey t, garcia-calvo m, houtzager vm, nordstrom pa, roy s, vaillancourt jp, chapman kt, nicholson dw (1997) a combinatorial approach defines specificities of members of the caspase family and granzyme b. functional relationships established for key mediators of apoptosis. j biol chem 272:17907–17911 3. yakovlev ag, knoblach sm, fan l, fox gb, goodnight r, faden ai (1997) activation of cpp32-like caspases contributes to neuronal apoptosis and neurological dysfunction after traumatic brain injury. j neurosci 17:7415–7424 4. clark rs, kochanek pm, watkins sc, chen m, dixon ce, seidberg na, melick j, loeffert je, nathaniel pd, jin kl, graham sh (2000) caspase-3 mediated neuronal death after traumatic brain injury in rats. j neurochem 74:740–753 5. s. m. knoblach, d. a. alroy et al, caspase inhibitor z-devd-fmk attenuates calpain and necrotic cell death in vitro and after traumatic brain injury, journal of cerebral blood flow & metabolism 24:1119–1132.
