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eIF4E-eIF4G inhibitor 4

Chemical Structure : eIF4E-eIF4G inhibitor 4

CAS No.:

eIF4E-eIF4G inhibitor 4

Catalog No.: PC-24502Not For Human Use, Lab Use Only.

eIF4E-eIF4G inhibitor 4 is a specific small molecule inhibitor of eukaryotic initiation factor 4E (eIF4E) with Kd of 0.09 uM, disrupts the eIF4E:eIF4G interaction with EC50 of 1.4 uM (SW620 cell).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

eIF4E-eIF4G inhibitor 4 is a specific small molecule inhibitor of eukaryotic initiation factor 4E (eIF4E) with Kd of 0.09 uM, disrupts the eIF4E:eIF4G interaction with EC50 of 1.4 uM (SW620 cell).
eIF4E-eIF4G inhibitor 4 demonstrates target engagement with eIF4E in intact cells (EC50=2 uM).
eIF4E-eIF4G inhibitor 4 only affects eIF4G (EC50 = 2.6 μM), but not 4E-BP1 binding to eIF4E.
eIF4E-eIF4G inhibitor 4 also significantly inhibits eIF4G:eIF4E binding between 1 and 10 µM in H1299 Non-small cell lung cancer (NSCLC) cell lysates (EC50=1.5 uM).
eIF4E-eIF4G inhibitor 4 significantly inhibited cap-dependent translation (EC50=4 uM) in vitro translation assay from HeLa cells.
eIF4E-eIF4G inhibitor 4 binds eIF4E in intact H1299 cells, shows clear dose-dependent thermal protection of eIF4E (EC50 = 2 uM).

Physicochemical Properties

M.Wt 347.43
Formula C20H26FNO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-2-((S)-1-(2'-fluoro-3-((2-hydroxyethyl)amino)-[1,1'-biphenyl]-4-yl)propoxy)propan-1-ol

References

1. Sharp SY, et al. Nat Commun. 2024 Nov 20;15(1):10037.

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