AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 μM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. AM 114 also exerts anti-cancer activity against cancer cells, which potently inhibits the growth of human colon cancer HCT116 cells with values of IC50 of 1.5 μM and 0.6 μM in MTT and colony formation assays respectively.
Reference
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