TAME 是后期促进复合体(APC/C 或 APC)的抑制剂,可与 APC/C 结合并阻止其通过 Cdc20 和 Cdh1 活化,产生有丝分裂阻滞。
产品描述
Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
体外活性
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. [1] TAME is hydrolysed by trypsin with Km of 0.328 mM. [2] TAME accelerates the ATP hydrolysis process about 12-fold. [3] TAME interacts with β and γ phosphate and the adenine ring of ATP by the guanidinium group and the aromatic ring. [4] TAME at concentration of 50 mM inhibits nutrient-induced germination and pressure-induced germination at 600 MPa in Bacillus subtilis. [5] TAME induces a concentration dependent contractile response on ileal strips with EC50 of 4.3 x 103 M. [6]
Cas No.
901-47-3
分子式
C14H22N4O4S
分子量
342.41
别名
N-4-Tosyl-L-arginine methyl ester;Tosylarginine methyl ester;N-[(4-甲基苯基)磺酰基]-L-精氨酸甲酯
储存和溶解度
DMSO:64 mg/mL (186.9 mM)
H2O:63 mg/mL (184 mM)
Ethanol:3 mg/mL (8.76 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years