eIF4A3 inhibitor 53a

eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Eukaryotic Initiation Factor (eIF)

IC50: 0.2 μM (eIF4A3)[1] Kd: 0.043 μM (eIF4A3)[1]

[1]. Ito M, et al. Discovery of Novel 1,4-Diacylpiperazines as Selective and Cell-Active eIF4A3 Inhibitors. J Med Chem. 2017 Apr 27;60(8):3335-3351.