(Z)-4EGI-1
目录号: PL14825 纯度: ≥98%
CAS No. :901787-88-0
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中文名称
(Z)-4EGI-1
中文别名
OTAVA-BB 7070707011
英文名称
(Z)-4EGI-1
英文别名
OTAVA-BB 7070707011;(Z)-4EGI-1;(αZ)-α-[2-[4-(3,4-Dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitrobenzenepropanoic acid (ACI);Benzenepropanoic acid, α-[[4-(3,4-dichlorophenyl)-2-thiazolyl]hydrazono]-2-nitro-, (αZ)- (9CI)
Cas No.
901787-88-0
分子式
C18H12Cl2N4O4S
分子量
451.28
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
(Z)-4EGI-1 是 4EGI-1 的 Z-型异构体,是 eIF4E/eIF4G 相互作用和翻译起始的抑制剂。(Z)-4EGI-1 有效结合 eIF4E ,IC50 为 43.5 μM,Kd 值为 8.74 μM。(Z)-4EGI-1 具有抗癌活性。
生物活性
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC 50 of 43.5 μM and a K d value of 8.74 μM. (Z)-4EGI-1 has anticancer activity.
性状
Solid
IC50 & Target[1][2]
eIF4
体外研究(In Vitro)
(Z)-4EGI-1 (15-30 μM; 6 hours; CRL-2813 melanoma cells) treatment markedly reduces the expressions of the regulatory proteins: cyclin D1, cyclin E, and Survivin, while the expressions of housekeeping proteins such as β-Actin and α-Tubulin are not affected.
(Z)-4EGI-1 inhibits cancer cells proliferation with IC50 values of 15.3 μM and 11.6 μM for CRL-2351 breast cells and CRL-2813 melanoma cells, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Khuloud Takrouri, et al. Structure-activity Relationship Study of 4EGI-1, Small Molecule eIF4E/eIF4G Protein-Protein Interaction Inhibitors. Eur J Med Chem. 2014 Apr 22;77:361-77.
[2]. Poornachandran Mahalingam, et al. Synthesis of Rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein-Protein Interaction. J Med Chem. 2014 Jun 26;57(12):5094-111.
溶解度数据
In Vitro: DMSO : 50 mg/mL (110.80 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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