中文名 | 4E1RCat |
英文名 | (E)-4-(3-((5-(4-Nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic |
别名 | 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 |
英文别名 | CS-1228 4E1RCat 4E1RCAT 4-[(3E)-3-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenylpyrrol-1-yl]benzoic acid (E)-4-(3-((5-(4-Nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic 4-[2,3-Dihydro-3-[[5-(4-nitrophenyl)-2-furanyl]methylene]-2-oxo-5-phenyl-1H-pyrrol-1-yl]benzoic acid 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 |
CAS | 328998-25-0 |
化学式 | C28H18N2O6 |
分子量 | 478.45 |
溶解度 | DMSO: ≥ 5 mg/mL |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | brown to dark brown |
体外研究 | 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. |
体内研究 | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.09 ml | 10.45 ml | 20.901 ml |
5 mM | 0.418 ml | 2.09 ml | 4.18 ml |
10 mM | 0.209 ml | 1.045 ml | 2.09 ml |
5 mM | 0.042 ml | 0.209 ml | 0.418 ml |
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