Apcin
| 中文名称 | Apcin |
|---|---|
| 中文同义词 | 2,2,2-三氯-1-(嘧啶-2-基氨基)乙基氨基甲酸2-(2-甲基-5-硝基-1H-咪唑-1-基)乙基;2-(2-甲基-5-硝基-1H-咪唑-1-基)乙基 (2,2,2-三氯-1-(嘧啶-2-基氨基)乙基)氨基甲酸酯;化合物APCIN;(2,2,2-三氯-1-(嘧啶-2-基氨基)乙基)氨基甲酸2-(2-甲基-5-硝基-1H-咪唑-1-基)乙酯;APCIN,CDC20抑制剂 |
| 英文名称 | Apcin |
| 英文同义词 | Apcin;3-(2-Methyl-5-nitroimidazol-1-yl)-N-(2,2,2-trichloro-1-phenylaminoethyl)propionamide;Carbamic acid, [2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester (9CI);Apcin >=98% (HPLC);2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl 2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethylcarbamate;2-(2-Methyl-5-nitro-1H-imidazol-1-yl)ethyl N-{2,2,2-trichloro-1-[(pyrimidin-2-yl)amino]ethyl}carbamate;ligase,pocket,anaphase-promoting,Apcin,recognition,complex,Inhibitor,Cdc20,Anaphase promoting complex,cyclosome,ubiquitylation,inhibit,mitosis,WD40-domain,APC/C,APC;Carbamic acid, N-[2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester |
| CAS号 | 300815-04-7 |
| 分子式 | C13H14Cl3N7O4 |
| 分子量 | 438.65 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 300815-04-7.mol |
| 结构式 |  |
Apcin 性质
| 密度 | 1.68±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | room temp |
| 溶解度 | DMF：25mg/mL； DMSO：25mg/mL； DMSO:PBS (pH 7.2) (1:1)：0.5 mg/mL |
| 酸度系数(pKa) | 9.67±0.46(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
Apcin (APC inhibitor) 是一种有丝分裂的 anaphase-promoting complex/cyclosome (APC/C) 的E3连接酶活性的抑制剂，其可与Cdc20结合并竞争性地抑制含D-box底物的泛素化。
| Target | Value |
|
APC/C
() | |
|
CDC20
() |
Apcin (25-50 μM; 48 hours) significantly increases MM apoptosis combining with proTAME (6, 12 μM).
Apcin (25 μM; 2-14 hours) induces slippage more slowly.
Apcin (50-200 μM) stabilizes cycB1-NT and securin most effectively, with somewhat weaker effects against full-length cyclin B1.
Apcin (1.5-200 μM; 18 hours) synergizes with proTAME (a cell-permeable TAME prodrug) to prolong mitotic duration in RPE1 cells.
Apoptosis Analysis
| Cell Line: | HMCLs LP-1 and RPMI-8226 cells |
| Concentration: | 25, 50 μM |
| Incubation Time: | 48 hours |
| Result: | Had minor effects on multiple myeloma (MM) cells alone and significantly increased MM apoptosis combining with proTAME (6, 12 μM). |
Western Blot Analysis
| Cell Line: | HeLa cells with Nocodazole (100 nM) |
| Concentration: | 25 μM |
| Incubation Time: | 2-14 hours |
| Result: | Induced slippage more slowly, as indicated by Cdc27 dephosphorylation and a reduction in cyclin B1, securin and phosphoH3 levels beginning 4-6h after mitotic entry. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-110287 | Apcin Apcin | 300815-04-7 | 5mg | 1000元 |
| 2024/04/30 | HY-110287 | Apcin Apcin | 300815-04-7 | 10mM * 1mLin DMSO | 1100元 |