proTAME

proTAME is a cell-permeable prodrug form of N-4-tosyl-L-arginine methyl ester (TAME; Item No. 17550), an inhibitor of the anaphase-promoting complex/cyclosome (APC/C), that is converted to TAME by intracellular esterases.^1,2 proTAME (12 μM) blocks association of APC/C with the activator CDH1 and inhibits degradation of APC/C substrates in HeLa cells.¹ It induces mitotic arrest in metaphase followed by cell death in synchronized HeLa H2B-GFP cells when used at a concentration of 12 μM. It also increases mitotic duration in asynchronous HeLa H2B-GFP cells at a concentration of 4 μM, an effect that is enhanced by knockdown of the APC/C co-activator CDC20. proTAME decreases the viability of several laboratory and primary patient-derived human multiple myeloma (MM) cell lines (IC₅₀s = 2.8-20.3 μM) and increases apoptosis in RPMI-8226, LP-1, NCI-H929, and U266 MM cells when used at a concentration of 12 μM.²

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1. Zeng, X., Sigoillot, F., Gaur, S., et al. Pharmacologic inhibition of the anaphase-promoting complex induces a spindle checkpoint-dependent mitotic arrest in the absence of spindle damage. Cancer Cell 18(4), 382-395 (2010).

2. Lub, S., Maes, A., De Veirman, K., et al. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells. Oncotarget 7(4), 4062-4076 (2016).