Apcin
| 中文名稱 | Apcin |
|---|---|
| 中文同義詞 | 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抑制劑;化合物APCIN,10 MM DMSO 溶液 |
| 英文名稱 | Apcin |
| 英文同義詞 | 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號 | 300815-04-7 |
| 分子式 | C13H14Cl3N7O4 |
| 分子量 | 438.65 |
| EINECS號 | |
| 相關(guān)類別 | 抑制劑 |
| Mol文件 | 300815-04-7.mol |
| 結(jié)構(gòu)式 |  |
Apcin 性質(zhì)
| 密度 | 1.68±0.1 g/cm3(Predicted) |
|---|---|
| 儲存條件 | room temp |
| 溶解度 | DMF：25mg/mL； DMSO：25mg/mL； DMSO:PBS (pH 7.2) (1:1)：0.5 mg/mL |
| 酸度系數(shù)(pKa) | 9.67±0.46(Predicted) |
| 形態(tài) | 粉末 |
| 顏色 | 白色至米色 |
| InChI | 1S/C13H14Cl3N7O4/c1-8-19-7-9(23(25)26)22(8)5-6-27-12(24)21-10(13(14,15)16)20-11-17-3-2-4-18-11/h2-4,7,10H,5-6H2,1H3,(H,21,24)(H,17,18,20) |
| InChIKey | ZEXHXVOGJFGTRX-UHFFFAOYSA-N |
| SMILES | CC1=NC=C([N+]([O-])=O)N1CCOC(NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)=O |
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。
| 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
| WGK Germany | WGK 3 |
|---|---|
| 存儲類別 | 11 - 可燃固體 |
| 危險性類別 | 眼部刺激 類別2 經(jīng)皮刺激 類別2 特異性靶器官毒性-一次接觸，類別3 |
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-110287 | Apcin | 300815-04-7 | 1 mg | 419元 |
| 2026/06/05 | HY-110287 | Apcin Apcin | 300815-04-7 | 5mg | 1000元 |