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Description: 4EGI-1 is a potent and competitive eIF4E/eIF4G interaction inhibitor which binds to eIF4E with KD of 25 uM. 4EGI-1 has been shown to amplify TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-induced apoptosis via down-regulation of FLIPS/L and induction of DR5. These characteristics of the compound seem to be independent of it's ability to inhibit cap-dependent protein translation which is caused by disruption of the eIF4E/eIF4G association through binding to eIF4E. It has been shown that while 4EGI-1 displaces eIF4G from eIF4E, it consequentially enhances 4E-BP association both in vivo and in vitro.
References: Cell. 2007 Jan 26; 128(2):257-67; Neoplasia. 2010 Apr; 12(4):346-56; Clin Cancer Res. 2013 Jun 15; 19(12):3212-23.
Chemical Name: alpha-[2-[4-(3, 4-Dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitro-benzenepropanoic acid
InChi Key: KFRKRECSIYXARE-HYARGMPZSA-N
InChi Code: InChI=1S/C18H12Cl2N4O4S/c19-12-6-5-10(7-13(12)20)15-9-29-18(21-15)23-22-14(17(25)26)8-11-3-1-2-4-16(11)24(27)28/h1-7, 9H, 8H2, (H, 21, 23)(H, 25, 26)/b22-14+
SMILES Code: O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2
4EGI-1; 4-EGI1; 4 EGI 1; 4EGI1; 4EGI1; 4 EGI1; 4-EGI-1
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