eIF4A3-IN-2

Research use only, not for human use.

eIF4A3-IN-2 is an allosteric, selective, non-competitive eIF4A3 inhibitor with IC50 of 0.11 uM.

eIF4A3-IN-2 is an allosteric, selective, non-competitive eIF4A3 inhibitor with IC50 of 0.11 uM, exhibits noncompetitive inhibition with ATP or RNA and high selectivity for eIF4A3 over other helicases; suppresses the helicase activity of eIF4A3 in an ATPase-dependent manner; targets the exon junction complex (EJC) and suppresses monsense-mediated mRNA decay.

eIF4A3-IN-2 (compound 2) binds to the allosteric region in eIF4A3 and inhibits in vitro ATPase, helicase, and cellular nonsense-mediated RNA decay (NMD) activities. Apoptosis Analysis Cell Line:HEK293T cells (transfected with the NMD reporter) luciferase assay Concentration:0.3, 1, 3, or 10 μM Incubation Time:3 or 6 h Result:eIF4A3-IN-2 induces an approximately 3.2-fold increase in luciferase activity, indicating that NMD is inhibited by compound 2.

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Nuclear Receptor/Transcription Factor

eIF

eIF

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2095677-20-4

602.711

C25H19Br2ClN4O2

>98% (HPLC)

DMSO : 100 mg/mL 165.92 mM

O=C(C1=CC=C(Br)C=C1)N2CCN(C(C3=C4N(C=C(Br)C=C4)N=C3)=O)C[C@@H]2C5=CC=C(Cl)C=C5

(S)-(4-(4-bromobenzoyl)-3-(4-chlorophenyl)piperazin-1-yl)(6-bromopyrazolo[1,5-a]pyridin-3-yl)methanone

(-20℃)

With Ice Pack

≥ 2 years