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Apcin
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Apcin图片
CAS NO:300815-04-7
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Apcin 是 Cdc20 的配体，是一种有效的竞争性后期促进复合物/环体 (APC/C(Cdc20)) E3 连接酶活性抑制剂。 Apcin 通过与 Cdc20 结合并阻止底物识别竞争性地抑制 APC/C 依赖性泛素化。 Apcin 占据 WD40 结构域侧面的 D-box 结合口袋，可以延长有丝分裂。
Cas No.300815-04-7
化学名[2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-carbamic acid, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester
Canonical SMILESCC1=NC=C([N+]([O-])=O)N1CCOC(NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)=O
分子式C13H14Cl3N7O4
分子量438.7
溶解度DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Apcin is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C). Apcin competitively binds to Cdc20 and prevents substrate interaction and ubiquitylation required for continuation of mitosis. Apcin enhances the effect of the APC/C inhibitor N-4-tosyl-L-arginine methyl ester and its prodrug, proTAME, leading to an increase in the number of cells in mitosis, a longer mitotic duration, and greater stabilization of cyclin B1, cycB1-NT, securin, and cyclin A2. Apcin, in combination with proTAME, synergistically increases apoptosis in multiple myeloma cells.

References:
[1]. Sackton, K.L., Dimova, N., Zeng, X., et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C Nature 514(7524), 646-649 (2014).
[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).