eIF4A3-IN-1 (compound 53a) 是一种选择性的真核起始因子 4A3 (eIF4A3) 抑制剂 (IC50=0.26 μM; Kd=0.043 μM)，eIF4A3-IN-1 与 eIF4A3 的非 ATP 结合位点结合，并在 10 μM 和 3 μM 时明显抑制细胞无义介导的 RNA 衰变 (NMD), 可作为进一步研究 eIF4A3、外显子连接复合体 (EJC) 和 NMD 的探针。
CAS：2095486-67-0
分子式：C29H23BrClN5O2
分子量：588.88
纯度：98%
存储：Store at -20°C

Background:

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]. 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.