Description
An inhibitor of chymotrypsin-like proteasome activity (IC50 = 27 nM); selective for the CTL activity over the TL and PGPH activities (IC50s = >100 µM for both), as well as for the 20S constitutive proteasome over the immunoproteasome (IC50s = 18 and 2,170 nM, respectively); decreases the viability of a panel of cancer cell lines (IC50s = 2.2-45.2 µM); induces cell cycle arrest at the G2/M phase, apoptosis, and autophagy, as well as inhibits migration and invasion, in U2OS and MG-63 cells at 40 and 60 µM, respectively; decreases tumor volume in an MDA-MB-231 breast cancer mouse xenograft model at 150 mg/kg