1000313-40-5

UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.

UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2].

[1] de Bruin G, et al. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem.?2014?Jul 24;57(14):6197-209. DOI:10.1021/jm500716s
[2] Wehenkel M, et al. A selective inhibitor of the immunoproteasome subunit LMP2 induces apoptosis in PC-3 cells and suppresses tumour growth in nude mice. Br J Cancer.?2012?Jun 26;107(1):53-62. DOI:10.1038/bjc.2012.243