TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor. In vitro
TAME inhibits cyclin proteolysis in mitotic Xenopus egg extract with IC50 of 12 µM. TAME at concentration of 1-200 μM arrests interphase extract treated with recombinant cyclin B1/Cdc2 complex in mitosis, with stable cyclin B1 and phosphorylated Cdc27. TAME at concentration of 200 μM dramaticly inhibits the ubiquitin ligase activity of the Anaphase-Promoting Complex (APC), accompanied by reduced binding of Cdh1 to APC. TAME addition to interphase extract reduces Cdc20 association with the APC in a dose-dependent manner partly by binding directly to APC, and the contribution motif is the C-terminal isoleucine-arginine (IR) tail on APC. TAME is hydrolysed by trypsin with Km of 0.328 mM. TAME accelerates the ATP hydrolysis process about 12-fold. TAME interacts with β and γ phosphate and the adenine ring of ATP by the guanidinium group and the aromatic ring. TAME at concentration of 50 mM inhibits nutrient-induced germination and pressure-induced germination at 600 MPa in Bacillus subtilis. TAME induces a concentration dependent contractile response on ileal strips with EC50 of 4.3 x 103 M.