AM114 is a chalcone derivative that inhibits chymotrypsin-like activity of the 20S proteasome with an IC50 value of about 1 μM. AM114 has the activity of inhibiting the growth of HCT116 p53+/+ cells with an IC50 value of 1.49 μM. AM114 has strong anticancer activity[1][2].Due to the inhibition of chymotrypsin-like activity of the 20S proteasome in vitro, AM114 leads to a massive accumulation of ubiquitinated p53 and other cellular proteins throughout the cell. At a concentration of 1µM for 14 days, AM114 reduced the viability of p53+/+ and p53-/- cells by approximately 70% and 20%, respectively. In contrast, AM114 caused apoptosis in 28% of HCT116 p53+/+ cells after 48 hours of action, and the proportion of apoptotic cells increased to 76% after 72 hours of treatment. In a colony formation assay, AM114 showed potent activity against p53+/+ cells carrying p53+/+ with an IC50 value of 0.6 µM[1].
搜索
