4EGI-1

Catalog No.S7369 Batch:S736901

Technical Data

Formula	C₁₈H₁₂Cl₂N₄O₄S
Molecular Weight	451.28	CAS No.	315706-13-9
Solubility (25°C)*	In vitro	DMSO	90 mg/mL (199.43 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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.

Targets

mTOR ^[4]	eIF4E/eIF4G ^[1] (Cell-free assay)
	25 μM(Kd)

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]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Jurkat cells and A549 lung cancer cells. Concentrations ~60 μM Incubation Time 24 hours Method 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.

Cell Assay:^{^[1]}

Cell lines
Jurkat cells and A549 lung cancer cells.
Concentrations
~60 μM
Incubation Time
24 hours
Method
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.

References

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

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Customer Product Validation

: 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's 4EGI-1 has been cited by 25 publications

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

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SHIPPING AND STORAGE
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