MG-101 (ALLN)

Description: MG-101 (also known as MG101; Calpain Inhibitor I and ALLN) is a novel, cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins with potential antitumor activity. It activates p53-dependent apoptosis in tumor cell lines. MG-101 inhibits calpain I, calpain II, cathepsin B and cathepsin L with Ki values of 190 nM, 220 nM, 150 nM and 500 pM, respectively. MG-101 combined with Ad/gTRAIL induced cell death dramatically in DLD1-TRAIL/R cells, while calpain alone had only minimal killing effects. It can reduce colon injury caused by dinitrobenzene sulphonic acid, overcome acquired resistance to TRAIL, protect against atractyloside-induced toxicity, and reduce colon injury caused by dinitrobenzene sulphonic acid.

References: Carcinogenesis. 1990 Jan; 11(1):75-80; J Biol Chem. 1991 Jul 15; 266(20):13311-7.