产品描述:
Potent and irreversible second-generation peptide epoxyketone class proteasome inhibitor. Synthetic analog of the microbial product epoxomicin (Prod. No. AG-CN2-0422). Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=5.2nM) and the beta5i subunit [LMP7] of the 20S immunoproteasome (IC50=14nM), with minimal cross-reactivity to other proteases. Displays equal potency but greater selectivity for the chymotrypsin-like activity of the proteasome compared to bortezomib (Prod. No. AG-CR1-3602). Anticancer compound effective against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma and various solid tumors (IC50s=2.4-20nM).