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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)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
APCin 是后期促进复合物/环体 (APC/C(Cdc20)) E3 连接酶活性的有效竞争性抑制剂,可通过与 Cdc20 结合并阻止底物识别竞争性地抑制 APC/C 依赖性泛素化。它占据 WD40 结构域侧面的 D-box 结合口袋,并可以延长有丝分裂。它通过阻断有丝分裂退出并通过共同添加 Ts-Arg-OMe 协同放大而起作用。

产品描述

Apcin is a potent and competitive inhibitor of anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. It acts by blocking mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe.

体外活性

apcin as a small molecule ligand of Cdc20 that inhibits APC/CCdc20 and prolongs mitosis.?apcin paradoxically shortens mitosis when SAC activity is high.?These opposing effects of apcin arise from targeting of a common binding site in Cdc20 required for both substrate ubiquitination and MCC-dependent APC/C inhibition.?Furthermore, apcin cooperates with p31comet to relieve MCC-dependent inhibition of APC/C.?Apcin therefore causes either net APC/C inhibition, prolonging mitosis when SAC activity is low, or net APC/C activation, shortening mitosis when SAC activity is high, demonstrating that a small molecule can produce opposing biological effects depending on regulatory context.

Cas No.

300815-04-7

分子式

C13H14Cl3N7O4

分子量

438.65

储存和溶解度

DMSO:240 mg/mL (547.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years