4E1RCAT
| 中文名称 | 4E1RCAT |
|---|---|
| 中文同义词 | 4-[2,3-二氢-3-[[5-(4-硝基苯基)-2-呋喃基]亚甲基]-2-氧代-5-苯基-1H-吡咯-1-基]苯甲酸;化合物4E1RCAT,10 MM DMSO 溶液;4E1RCat试剂;4E1RCat试剂 |
| 英文名称 | 4E1RCat |
| 英文同义词 | 4E1RCat;Benzoic acid, 4-[2,3-dihydro-3-[[5-(4-nitrophenyl)-2-furanyl]Methylene]-2-oxo-5-phenyl-1H-pyrrol-1-yl]-;4-[(3E)-3-[[5-(4-Nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl]benzoic acid;4-[(3E)-3-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenylpyrrol-1-yl]benzoic acid;4-[2,3-Dihydro-3-[[5-(4-nitrophenyl)-2-furanyl]methylene]-2-oxo-5-phenyl-1H-pyrrol-1-yl]benzoic acid;CS-1228;inhibit,Inhibitor,4E-1rcat,4E1rcat,Eukaryotic Initiation Factor (eIF),Autophagy;4-(3-((5-(4-Nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acid |
| CAS号 | 328998-25-0 |
| 分子式 | C28H18N2O6 |
| 分子量 | 478.45 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;小分子抑制剂;抑制剂;医药;Inhibitors |
| Mol文件 | 328998-25-0.mol |
| 结构式 |  |
4E1RCAT 性质
| 沸点 | 764.8±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.423±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥5mg/mL |
| 酸度系数(pKa) | 4.23±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 棕色至深棕色 |
| InChI | 1S/C28H18N2O6/c31-27-21(16-24-14-15-26(36-24)19-6-12-23(13-7-19)30(34)35)17-25(18-4-2-1-3-5-18)29(27)22-10-8-20(9-11-22)28(32)33/h1-17H,(H,32,33)/b21-16+ |
| InChIKey | BBQRBOIMSKMFFO-LTGZKZEYSA-N |
| SMILES | OC(=O)c1ccc(cc1)N2C(=O)\C(=C\c3ccc(o3)-c4ccc(cc4)[N+]([O-])=O)C=C2c5ccccc5 |
IC50: ∼4 μM (eIF4E/eIF4G)
4E1RCat is an inhibitor of eIF4E:eIF4GI interaction, with an IC 50 an of ∼4 μM. 4E1RCat binding to eIF4E also interferes with eIF4G and 4E-BP binding. 4E1RCat inhibits ribosome recruitment to mRNA in a cap-dependent manner. 4E1RCat blocks the capped mRNA translation, and the translation is activated by CDK1/CYCB1. Nearly all new protein synthesis in both mitosis and interphase is cap-dependent and -sensitive to 4E1RCat treatment, in HeLa and U2OS cells.
4E1RCat (15 mg/kg, i.p.) affacts chemosensitivity of Pten +/- Eμ-Myc tumors in mice. 4E1RCat (15 mg/kg, i.p.) sensitizes Pten +/- Eμ-Myc and Tsc2 +/- Eμ-Myc lymphomas to the cytotoxic effects of doxorubicin (Dxr), and 4E1RCat targets translation in mice.
安全信息
| WGK Germany | 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-14427 | 4E1RCat | 328998-25-0 | 1 mg | 363元 |
| 2026/09/15 | HY-14427 | 4E1RCAT 4E1RCat | 328998-25-0 | 5mg | 800元 |