Small-molecule inhibitor: PF3491390

Name

History: The history of the development of IDN-6556 was described by Linton et al. (2005).
Peptidases inhibited: Caspases (family C14) including caspase-1, caspase-3 and caspase-7. This is a broad-spectrum caspase inhibitor. Only at high micromolar concentrations is there inhibition of papain, calpain, cathepsin B or chymotrypsin (Linton et al., 2005).
Mechanism: Inhibition is irreversible.
Pharmaceutical relevance: IDN-6556 blocks apoptosis, and has been subjected to clinical trials in patients undergoing liver transplantation and other solid organ transplantation with a view to preventing reperfusion injury (Leung-Toung et al., 2006).

Structure
Chemical/biochemical name: 3-[2-(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3 ,5,6-tetrafluoro-phenoxy)-pentanoic acid

Comment: IDDN-6556 is an oxamyl-dipeptide and tetrafluorophenoxy methyl ketone (Linton et al., 2005).
Reviews: Linton et al. (2005)