MG-101

110044-82-1

C20H37N3O4

DMSO : 16.67 mg/mL (43.46 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Metabolic Enzyme/Protease

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 uM) that activates p53-dependent apoptosis in tumor cell lines. At 10-100 uM MG-101 dose-dependently prevents the degradation of IkappaBalpha and IkappaBbeta by the ubiquitin-proteasome complex, which blocks activation of NFkappaB and the production of TNF and IL-1beta, suggesting a potential therapeutic effect for inflammatory diseases.2 At 10 uM, 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]