EIF4A3-IN-1

EIF4A3-IN-1 is a selective eIF4A3 inhibitor (IC50: 0.26 μM; Kd: 0.043 μM) with cellular nonsense-mediated RNA decay (NMD) inhibitory activity. eIF4A3-IN-1 can specifically bind to the non-ATP binding site of eIF4A3. eIF4A3-IN-1 has anti-tumor and analgesic activities[1][2][3].

Product Specifications

CAS Number

[2095486-67-0]

UNSPSC

12352005

Target

Eukaryotic Initiation Factor (eIF)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/eif4a3-in-1.html

Purity

99.96

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

ClC(C=C1)=CC=C1[C@@H]2N(C(C3=CC=C(Br)C=C3)=O)CCN(C(C4=C(C)N(C5=CC=CC(C#N)=C5)N=C4)=O)C2

Molecular Formula

C29H23BrClN5O2

Molecular Weight

588.88

References & Citations

[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.|[2]López-Cánovas JL, et al. Spliceosomal profiling identifies EIF4A3 as a novel oncogene in hepatocellular carcinoma acting through the modulation of FGFR4 splicing. Clin Transl Med. 2022 Nov;12 (11) :e1102.|[3]Hsieh MC, et al. Phosphorylated Upstream Frameshift 1-dependent Nonsense-mediated μ-Opioid Receptor mRNA Decay in the Spinal Cord Contributes to the Development of Neuropathic Allodynia-like Behavior in Rats. Anesthesiology. 2023 Jun 1;138 (6) :634-655.