eIF4A3-IN-1

• CAT Number: I018774
• CAS Number: 2095486-67-0
• Molecular Formula: C29H23BrClN5O2
• Molecular Weight: 588.88
• Purity: ≥95%
• Synonyms: 3-[4-[(3S)-4-(4-bromobenzoyl)-3-(4-chlorophenyl)piperazine-1-carbonyl]-5-methylpyrazol-1-yl]benzonitrile
• InChI: InChI=1S/C29H23BrClN5O2/c1-19-26(17-33-36(19)25-4-2-3-20(15-25)16-32)29(38)34-13-14-35(28(37)22-5-9-23(30)10-6-22)27(18-34)21-7-11-24(31)12-8-21/h2-12,15,17,27H,13-14,18H2,1H3/t27-/m1/s1
• InChIKey: BDGKKHWJYBQRIE-HHHXNRCGSA-N
• SMILES: CC1=C(C=NN1C2=CC=CC(=C2)C#N)C(=O)N3CCN(C(C3)C4=CC=C(C=C4)Cl)C(=O)C5=CC=C(C=C5)Br

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].

Reference

[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.
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