4EGI-1

製品コードS7369 バッチS736902

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₂Cl₂N₄O₄S

分子量

451.28

CAS No.

315706-13-9

Solubility (25°C)*

体外

DMSO

45 mg/mL (99.71 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 PBS

4.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of PBS and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with K_D of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.
in vitro	4EGI-1 disrupts the eIF4F complex and inhibits Cap-dependent translation in vitro. 4EGI-1 has proapoptotic activity in Jurkat cells, and potently inhibits cell growth with IC50 of approximately 6 μM in A549 lung cancer cells. ^[1] 4EGI-1 augments TRAIL-induced apoptosis through induction of DR5 and down-regulation of c-FLIP, independent of inhibition of cap-dependent protein translation in human lung cancer cells. ^[2] In addition, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. ^[3]

製品説明

4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with K_D of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.

in vitro

4EGI-1 disrupts the eIF4F complex and inhibits Cap-dependent translation in vitro. 4EGI-1 has proapoptotic activity in Jurkat cells, and potently inhibits cell growth with IC50 of approximately 6 μM in A549 lung cancer cells. ^[1] 4EGI-1 augments TRAIL-induced apoptosis through induction of DR5 and down-regulation of c-FLIP, independent of inhibition of cap-dependent protein translation in human lung cancer cells. ^[2] In addition, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Jurkat cells and A549 lung cancer cells.
	濃度	~60 μM
	反応時間	24 hours
	実験の流れ	Cell viability is measured by treatment of Jurkat cells with compound for 24 h and by determination of intracellular ATP using the CellTiterGlo assay. For measurement of apoptotic DNA fragmentation, cells are treated for 24 h with 60 μM EGI-1 or 6.65 μM camptothecin in the presence or absence of 100 mM zVAD-FMK, a broad-spectrum caspase inhibitor. After fixation and staining with PI, cellular DNA content is determined by FACS analysis in a FACS Calibur machine. Nuclear morphology after 24 h EG1-1 treatment is visualized by staining of cells with Hoechst dye and ﬂuorescence microscopy. For the A549 lung cancer cells, cell growth in the presence of 4EGI-1 is determined using the SRB staining method.

参考

[4] Jin Young Sung, et al. Exp Gerontol . 2018 Aug;109:51-58.

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カスタマーフィードバック

: Data from [Data independently produced by , , Mol Cancer Ther, 2017, 16(9):1806-1818]

: Data from [Data independently produced by , , Int J Oncol, 2015, 47(6):2217-25.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

DEAD-Box Helicase 17 Promotes Amyloidogenesis by Regulating BACE1 Translation [ Brain Sci, 2023, 13(5)745]	PubMed: 37239217
DEAD-Box Helicase 17 Promotes Amyloidogenesis by Regulating BACE1 Translation [ Brain Sci, 2023, 13(5)745]	PubMed: 37239217
Surgical Reconstruction of Stage 3 and 4 Pressure Injuries: A Literature Review and Proposed Algorithm from an Interprofessional Working Group [ Adv Skin Wound Care, 2023, 36(5):249-258]	PubMed: 37079788
Ribosome Quality Control Mechanism Mitigates the Cytotoxic Impacts of Ribosome Collisions Induced by 5-Fluorouracil [ bioRxiv, 2023, 10.1101/2023.12.26.573247]	PubMed: none
Dephosphorylation of 4EBP1/2 Induces Prenatal Neural Stem Cell Quiescence [ bioRxiv, 2023, 2023.02.14.528513]	PubMed: 36824760
Retinoic acid and RARγ maintain satellite cell quiescence through regulation of translation initiation [ Cell Death Dis, 2022, 13-9:838]	PubMed: 36175396
Role of EIF4G1 network in non-small cell lung cancers (NSCLC) cell survival and disease progression [ J Cell Mol Med, 2021, 10.1111/jcmm.16307]	PubMed: 33539648
TUFM is involved in Alzheimer's disease-like pathologies that are associated with ROS [ FASEB J, 2021, 35(5):e21445]	PubMed: 33774866
Berberine Represses β-Catenin Translation Involving 4E-BPs in Hepatocellular Carcinoma Cells [ Mol Pharmacol, 2021, 99(1):1-16]	PubMed: 33130557
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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