2. Cell Cycle/DNA Damage Apoptosis GPCR/G Protein MAPK/ERK Pathway
  3. Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Ras PERK
  4. eIF4E/eIF4G PPI-IN-1

eIF4E/eIF4G PPI-IN-1 是一种 eIF4E/eIF4G 相互作用抑制剂，对 eIF4E 蛋白的 KD 为 20.2 μM。eIF4E/eIF4G PPI-IN-1 通过多种作用模式发挥抗肿瘤作用，包括通过抑制 Ras/MAPK/eIF4E 信号通路来调节 eIF4E 的活性、细胞凋亡 (apoptosis) 和细胞迁移。eIF4E/eIF4G PPI-IN-1 可抑制裸鼠 HepG2 异种移植瘤的生长，并且对小鼠相对无毒。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

eIF4E/eIF4G PPI-IN-1 Chemical Structure

eIF4E/eIF4G PPI-IN-1 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

eIF4E/eIF4G PPI-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

查看 Ras 亚型特异性产品:

查看所有亚型
K-Ras H-Ras N-Ras Ras

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice[1].

IC50 & Target

eIF4E

20.2 μM (Kd)

eIF4G

 

Bcl-2

 

体外研究
(In Vitro)

eIF4E/eIF4G PPI-IN-1 (Compound A37) (25 μM) 对癌细胞系 A549、Hela、HepG2 和 MCF-7 表现出抑制活性，抑制率分别为 98.08、81.74、100.78 和 78.52[1]。

eIF4E/eIF4G PPI-IN-1 可抑制 A549、Hela、HepG2 和 MCF-7 癌细胞的增殖，IC50 值分别为 4.59 μM，2.69 μM，2.22 μM 和 3.45 μM [1]。

eIF4E/eIF4G PPI-IN-1 在 HEK-293T 细胞中表现出较低的细胞毒性 (IC50 ; 40 μM)[1]。

eIF4E/eIF4G PPI-IN-1 (1-5 μM, 48 h) 通过调节 HepG2 细胞中 Bcl-2、Bax 和 C-Caspase-3 蛋白的表达来诱导癌细胞凋亡[1]。

eIF4E/eIF4G PPI-IN-1 (2.5 μM, 12 h, 24 h) 抑制 HepG2 细胞迁移[1]。

eIF4E/eIF4G PPI-IN-1 (1-5 μM, 48 h) 不会在 HepG2 细胞中诱导明显的细胞周期停滞[1]。

eIF4E/eIF4G PPI-IN-1 (1-5 μM, 48 h) 通过抑制 HepG2 细胞中 Ras、p-MNK、p-ERK 和 p-eIF4E 的表达发挥抗肿瘤作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

eIF4E/eIF4G PPI-IN-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: HepG2 cell
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Induced 49 % apoptosis of HepG2 cells at 2.5 μM.
Induced HepG2 cells apoptosis over 74 % at 5.0 μM.

Cell Migration Assay [1]

Cell Line: HepG2 cell
Concentration: 2.5 μM
Incubation Time: 12 h, 24 h
Result: Suppressed HepG2 cell migration.

Cell Cycle Analysis[1]

Cell Line: HepG2 cell
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Did not induce significant cell cycle arrest, but increased the G0/G1 phase population at 5 μM.

Western Blot Analysis[1]

Cell Line: HepG2 cell
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Down-regulated the expression of anti-apoptotic protein Bcl-2 and up-regulated the expression of pro-apoptotic genes Bax and C-Caspase-3.
Inhibited the expression of Ras, p-MNK, p-ERK and p-eIF4E.
体内研究
(In Vivo)

eIF4E/eIF4G PPI-IN-1 (Compound A37) (25 mg/kg，50 mg/kg，腹腔注射，每日一次，18 天) 抑制 HepG2 异种移植肿瘤小鼠模型中 HepG2 细胞的生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HepG2(1 × 107, s.c.) xenograft tumor on the seven-week-old female Balb/c nude mice weighing 16-19 g. mice model[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: i.p., once a day,18 days
Result: Reduced tumor growth, did not change weight and the shape of organ tissues.
分子量

430.31

Formula

C20H13Cl2N3O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

eIF4E/eIF4G PPI-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

eIF4E/eIF4G PPI-IN-1Eukaryotic Initiation Factor (eIF)Bcl-2 FamilyApoptosisRasPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseInhibitorHela cellHepG2 cellMCF-7 cellHEK-293T cellHepG2 xenograft tumor mice modelinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
eIF4E/eIF4G PPI-IN-1
目录号：
HY-176288
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z