4E1rcat ( eIF4E/eIF4G Interaction Inhibitor II )

产品货号. M14080 CAS No. 328998-25-0

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

4E1rcat
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

4E1RCat 是 eIF4E:eIF4G 和 eIF4E:4E-BP1 相互作用的双重抑制剂，并抑制 eIF4G 与 eIF4E 的结合，IC50 为 3.2 μM。
产品描述

4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM.
体外实验

4E1RCat is an inhibitor of eIF4E:eIF4GI interaction, with an IC50 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.
体内实验

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.
同义词

eIF4E/eIF4G Interaction Inhibitor II
通路

Apoptosis
靶点

PERK
受体

eIF-4E| eIF-4G
研究领域

Cancer
适应症

——

CAS Number

328998-25-0
分子量

478.45
分子式

C28H18N2O6
纯度

>98% (HPLC)
溶解度

DMSO: 96 mg/mL (200.64 mM)
SMILES

O=C1/C(C=C(C2=CC=CC=C2)N1C3=CC=C(C(O)=O)C=C3)=C\C4=CC=C(C5=CC=C([N+]([O-])=O)C=C5)O4
化学全称

(Z)-4-(3-((5-(4-nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acid

1.Shuda M, et al. Proc Natl Acad Sci U S A. 2015 May 12;112(19):5875-82.

计算器

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