N-[(4-甲基苯基)磺酰基]-L-精氨酸甲酯
中文名称 | N-[(4-甲基苯基)磺酰基]-L-精氨酸甲酯 |
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中文同义词 | N-[(4-甲基苯基)磺酰基]-L-精氨酸甲酯;NA-P-甲苯磺基-L-精氨酸甲酯;TAME,APC抑制剂 |
英文名称 | P-TOLUENESULFONYL-L-ARGININE METHYL ESTER HCL |
英文同义词 | Tosylarginine Methyl Ester;Nα-(4-Methylphenylsulfonyl)-L-arginine methyl ester;Nα-(p-Tolylsulfonyl)-L-arginine methyl ester;Nα-Tosylarginine methyl ester;Nα-Tosyl-L-arginine methyl;Nα-Tosyl-L-arginine methyl ester;(S)-methyl 5-guanidino-2-(4-methylphenylsulfonamido)pentanoate;TOSYL-L-ARGININE METHYL ESTER |
CAS号 | 901-47-3 |
分子式 | C14H22N4O4S |
分子量 | 342.41 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;细胞周期;Inhibitors |
Mol文件 | 901-47-3.mol |
结构式 |
N-[(4-甲基苯基)磺酰基]-L-精氨酸甲酯 性质
沸点 | 516.5±60.0 °C(Predicted) |
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密度 | 1.34 |
储存条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 | ≥ 17.1mg/mL,溶于 DMSO |
酸度系数(pKa) | 9.06±0.50(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
Anaphase-promoting complex (APC)
The absence of APC substrates, TAME ejects Cdc20 from the APC by promoting Cdc20 auto-ubiquitination in its N-terminal region. Cyclin B1 antagonizes TAME's effect by promoting binding of free Cdc20 to the APC and suppressing Cdc20 auto-ubiquitination.
TAME stabilizes cyclin B1 in
Xenopus
extract by two mechanisms. First, it reduces the k
cat
of the APC
Cdc20
/cyclin B1 complex without affecting the K
m
, slowing the initial ubiquitination of unmodified cyclin B1. Second, as cyclin B1 becomes ubiquitinated, it loses its ability to promote Cdc20 binding to the APC in the presence of TAME. As a result, cyclin B1 ubiquitination terminates before reaching the threshold necessary for proteolysis.