300815-04-7
中文名稱
Apcin
英文名稱
Apcin
CAS
300815-04-7
分子式
C13H14Cl3N7O4
分子量
438.65
MOL 文件
300815-04-7.mol
更新日期
2024/11/08 11:24:23
300815-04-7 結(jié)構(gòu)式
基本信息
中文別名
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 英文別名
ApcinApcin >=98% (HPLC)
3-(2-Methyl-5-nitroimidazol-1-yl)-N-(2,2,2-trichloro-1-phenylaminoethyl)propionamide
2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl 2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethylcarbamate
Carbamic acid, [2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester (9CI)
物理化學性質(zhì)
密度1.68±0.1 g/cm3(Predicted)
儲存條件room temp
溶解度DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
酸度系數(shù)(pKa)9.67±0.46(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
Apcin (APC inhibitor) 是一種有絲分裂的 anaphase-promoting complex/cyclosome (APC/C) 的E3連接酶活性的抑制劑，其可與Cdc20結(jié)合并競爭性地抑制含D-box底物的泛素化。靶點
| Target | Value |
|
APC/C
() | |
|
CDC20
() |
體外研究
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. |