AM 114

Uses

AM 114 induces significant cytotoxic effect in cancer cells through the inhibition of the cellular proteasome and provide a rationale for the further development of this class of compounds as novel cancer chemotherapeutic agents.

Biological Activity

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.achanta g, modzelewska a, feng l, khan sr, huang p. a boronic-chalcone derivative exhibits potent anticancer activity through inhibition of the proteasome. mol pharmacol. 2006 jul;70(1):426-33. epub 2006 apr 24.