Formulation: A solution in methyl acetate
Formal Name: (2S)-2-[[(4-methylphenyl)sulfonyl]amino]-9,13-dioxo-14-phenyl-7-[[[[(2-phenylacetyl)oxy]methoxy]carbonyl]amino]-10,12-dioxa-6,8-diazatetradec-6-enoic acid, methyl ester
Purity: ≥90%
Formula Markup: C34H38N4O12S
Formula Weight: 726,8
Shelf life (days): 730
CAS Number: 1362911-19-0
Notes: 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.{28533,36286} proTAME (12 μM) blocks association of APC/C with the activator CDH1 and inhibits degradation of APC/C substrates in HeLa cells.{28533} 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.{36286}
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