proTAME

A cell-permeable prodrug form of TAME; is converted to TAME by intracellular esterases; blocks association of APC/C with the activator CDH1 and inhibits degradation of APC/C substrates in HeLa cells at 12 µM; induces mitotic arrest in metaphase followed by cell death in synchronized HeLa H2B-GFP cells at 12 µM; increases mitotic duration in asynchronous HeLa H2B-GFP at 4 µM, an effect that is enhanced by knockdown of the APC/C co-activator CDC20; decreases the viability of several laboratory and primary patient-derived human MM cell lines (IC50s = 2.8-20.3 µM); increases apoptosis in RPMI-8226, LP-1, NCI-H929, and U266 MM cells at 12 µM