An inhibitor of eIF4A3
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eIF4A3-IN-1

Item No. 45609

Technical Information
Formal Name
3-[4-[[(3S)-4-(4-bromobenzoyl)-3-(4-chlorophenyl)-1-piperazinyl]carbonyl]-5-methyl-1H-pyrazol-1-yl]-benzonitrile
CAS Number
2095486-67-0
Synonyms
  • eIF4A-III-IN-1
  • eIF4A3 Inhibitor 1
  • Eukaryotic Initiation Factor 4A3 Inhibitor 1
  • Eukaryotic Initiation Factor 4A-III Inhibitor 1
  • T-202
Molecular Formula
C29H23BrClN5O2
Formula Weight
Purity
≥95%
A solid
SMILES
O=C(C1=CC=C(C=C1)Br)N2[C@@H](C3=CC=C(C=C3)Cl)CN(CC2)C(C4=C(N(C5=CC(C#N)=CC=C5)N=C4)C)=O
InChi Code
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
InChi Key
BDGKKHWJYBQRIE-HHHXNRCGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    eIF4A3-IN-1 is an inhibitor of eukaryotic initiation factor 4A-III (eIF4A3).1 It selectively inhibits the ATPase activity of eIF4A3 (IC50 = 0.26 µM) over the ATPase activities of eIF4A1, eIF4A2, DExH-box protein DHX29, and RNA helicase Brr2 (IC50s = >100 µM for all). eIF4A3-IN-1 inhibits nonsense-mediated RNA decay (NMD) in HEK293 cells at 10 µM and reduces proliferation, colony formation, and tumorsphere size in HepG2, Hep3B, and SNU-387 hepatocellular carcinoma cells at 3 nM.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ito, M., Tanaka, T., Cary, D.R., et al. Discovery of novel 1,4-diacylpiperazines as selective and cell-active eIF4A3 inhibitors. J. Med. Chem. 60(8), 3335-3351 (2017).

    2. López-Cánovas, J.L., Hermán-Sánchez, N., Moreno-Montilla, M.T., et al. Spliceosomal profiling identifies EIF4A3 as a novel oncogene in hepatocellular carcinoma acting through the modulation of FGFR4 splicing. Clin. Transl. Med. 12(11), e1102 (2022).