Caspase-2 is a cysteine protease that plays a key role in apoptosis, but appears to have multiple functions beyond cell death. Many aspects of caspase-2 activation and function remain unclear, but it appears that it acts both as an activator and inhibitor of apoptosis. Caspase-2 inhibitors are vital to studies to better understand the role caspase-2 plays in various disease states and are being studied as potential therapeutic targets for disorders involving apoptosis such as Alzheimer’s and Huntington’s. The fluor-methyl peptide inhibitor, VDVAD-FMK, is one of the most well-known capsase-2 inhibitors but several other peptide and small molecule inhibitors are available for this target.