4E1RCat | eIF4E/eIF4G Interaction Inhibitor II | eIF Inhibitor

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4E1RCat {[allProObj[0].p_purity_real_show]}

货号：A940826 同义名： eIF4E/eIF4G Interaction Inhibitor II

4E1RCat抑制eIF4E:eIF4G和eIF4E:4E-BP1的相互作用，防止eIF4F复合物的组装，抑制帽依赖性翻译，IC50约为4 μM。

4E1RCat 化学结构
CAS号：328998-25-0

4E1RCat 3D分子结构
CAS号：328998-25-0

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4E1RCat 纯度/质量文件产品仅供科研

货号：A940826 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

4E1RCat 生物活性

描述

Eukaryotic translation initiation is tightly regulated at the step of ribosome recruitment. This process involves binding of eukaryotic initiation factor (eIF) 4F complex to mRNA cap structures. eIF4F is composed of: eIF4E, the cap-binding protein; eIF4A, a DEAD-box RNA helicase; and eIF4G, a scaffolding protein that bridges the interaction between eIF4E and eIF4A. 4E1RCat is an inhibitor of eIF4E:eIF4G interaction with an IC₅₀ an of ∼4 μM. It also blocks eIF4E:4E-BP1 interaction. 4E1RCat at 50 μM reduced 80S ribosome complex formation and this inhibition of ribosome recruitment to mRNA by 4E1RCat was cap-specific. 4E1RCat inhibited cap-dependent translation from FF/HCV/Ren in a dose dependent manner. It also inhibited cap-dependent production of Ren Luc from Ren/CrPV/FF. Furthermore, in Jurkat cells, 4E1RCat at 50 μM decreased polysomes, increased the fraction of 80S ribosomal subunits, and decreased levels of Mcl-1 and c-Myc proteins, two eIF4E-dependent mRNAs. In vivo, 4E1RCat (15 mg/kg daily for 5 d) could reverse chemoresistance in a Myc-driven lymphoma model, consistent with the idea that deregulated translation plays a role in this phenomenon^[3].

作用机制

eIF4E has five shallow pockets that form an elongated binding site and could support small molecule interactions. 4E1RCat shows potential for binding to four of these pockets^[3].

4E1RCat 参考文献

[1]Salomon JJ, Spahn S,et al. Generation and functional characterization of epithelial cells with stable expression of SLC26A9 Cl- channels. Am J Physiol Lung Cell Mol Physiol. 2016 Apr 1;310(7):L593-602.

[2]Muanprasat C, Sonawane ND, et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004 Aug;124(2):125-37.

[3]Cencic R, Hall DR, Robert F, et al. Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F. Proc Natl Acad Sci U S A. 2011;108(3):1046-1051

4E1RCat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.04mL

20.90mL

4.18mL

2.09mL

4E1RCat 技术信息

CAS号	328998-25-0
分子式	C₂₈H₁₈N₂O₆
分子量	478.452

别名	eIF4E/eIF4G Interaction Inhibitor II
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 16 mg/mL(33.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

4E1RCat {[allProObj[0].p_purity_real_show]}

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