Carfilzomib (PR-171) is a potent, highly selective inhibitor chymotrypsin-like activity of proteasome with IC50 of 6 nM.
Carfilzomib (PR-171) weakly inhibits caspase-like and trypsin-like activities in cellular assays (IC50150-200 nM), also inhibits the chymotrypsin-like activity of the immunoproteasome (IC50=33 nM).
Carfilzomib (PR-171) accumulates proteasome substrates and induces cell cycle arrest and/or apoptosis.
Carfilzomib (PR-171) shows antitumor efficacy in vivo.
