MG-101 NLT 98%

MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). IC50 value: 150 nM (Ki) Target: cysteine protease in vitro: MG-101 is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines. At 10-100 μM MG-101 dose-dependently prevents the degradation of IκBα and IκBβ by the ubiquitin-proteasome complex, which blocks activation of NFκB and the production of TNF and IL-1β, suggesting a potential therapeutic effect for inflammatory diseases.2 At 10 μM, MG-101 can inhibit nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene. In HCT116 cells, MG-101 decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria. [1] in vivo: In mice bearing HCT116 xenografts, MG-101 (10 mg/kg i.p.) inhibits colon tumor formation. [1]