A successful virtual screening experiment of novel SIRT2 inhibitors is described. Four out of 11experimentally tested compounds showed in vitro inhibitory activity toward SIRT2 in a micromolar level,resulting in an experimental hit ratio of 36%. Two of these compounds inhibited SIRT2 with IC50 (μM)values of 51 and 91; moreover, one of the new inhibitors was comprised of an entirely new SIRT2-inhibitingstructural scaffold.