Home Cell Cycle eIF inhibitor - mTOR inhibitor - Apoptosis related activator 4EGI-1 For research use only.

4EGI-1

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

4EGI-1 Chemical Structure

4EGI-1 Chemical Structure

CAS No. 315706-13-9

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4EGI-1 Related Products

Biological Activity

Description 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD 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
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]
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 451.28 Formula

C18H12Cl2N4O4S
CAS No. 315706-13-9 SDF Download 4EGI-1 SDF
Smiles C1=CC=C(C(=C1)CC(=NNC2=NC(=CS2)C3=CC(=C(C=C3)Cl)Cl)C(=O)O)[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (199.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
We were wondering if you had data on the racemic mixture composition of this compound. Specifically, the ratio of E to Z enantiomers.

Answer:
The ratio of E to Z form is about 94.6 : 4.7. Please kindly find the HPLC enclosed, in which the E and Z form are seperated.

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