产品
编 号:F622265
分子式:C10H14Cl3N5O2
分子量:342.61
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
2640
In-stock
1mg
960
In-stock
5mg
2400
In-stock
10mg
3600
In-stock
25mg
询价
In-stock
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产品详情
生物活性:
Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257).

体外活性:
Apcin-A (25 μM;10 h) 显著降低 HCT116 和 HeLa 细胞中 Nocodazole (HY-13520) 诱导的有丝分裂分数,加速 cyclin B1 降解和 CDC27 的磷酸化,并促进有丝分裂滑脱。 Apcin-A (500 μM;5 min) 在重组系统中与 p31comet 协同减少 MCC 与 APC/C 的结合,缓解 MCC 对 APC/C 的抑制。 Apcin-A (200 μM;10 h) 抑制 Xenopus 卵提取物中 APC/C 介导的 securin 和 cyclin B1 泛素化及降解。

产品资料