| S0706 |
ISRIB
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ISRIB is an integrated stress response (ISR) inhibitor that potently reverses the effects of eukaryotic initiation factor 2α (eIF2α) phosphorylation.
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EMBO J, 2025, 44(4):1107-1130
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Cell Death Dis, 2025, 16(1):190
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Cancer Cell Int, 2025, 25(1):245
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| S8994 |
Zotatifin (eFT226)
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Zotatifin (eFT226) is a highly effective and sequence-selective inhibitor of the RNA helicase eIF4A. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5'-UTRs, with an IC50 of 2 nM, and disrupts the assembly of the eIF4F initiation complex. By enhancing the interaction between eIF4A and polypurine RNA sequence or structural motifs, zotatifin converts eIF4A into a sequence-specific translation repressor, thereby regulating the translation of certain target genes. It also exhibits anti-tumor activity.
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| S8275 |
Tomivosertib (eFT-508)
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Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. This compound inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
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Nat Commun, 2025, 16(1):7853
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Nat Commun, 2024, 15(1):9755
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Nat Commun, 2024, 15(1):9755
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| S7369 |
4EGI-1
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4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. This compound specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. It induces apoptosis.
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Nat Commun, 2024, 15(1):4083
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Nat Commun, 2024, 15(1):4083
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Nucleic Acids Res, 2024, gkae849
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| S7370 |
4E1RCat
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4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E.
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Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
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Cell Chem Biol, 2021, S2451-9456(21)00213-0
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J Cell Mol Med, 2021, 10.1111/jcmm.16307
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| S8181 |
SBI-0640756
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SBI-0640756(SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex. It can also suppress AKT and NF-κB signaling.
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Neoplasia, 2024, 60:101109
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Sci Rep, 2021, 11(1):21689
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| S6533 |
Briciclib
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Briciclib (ON-014185) is a water soluble derivative of ON-013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E).
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| S2923 |
Salubrinal
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Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
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Cell Discov, 2025, 11(1):80
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Cell Metab, 2025, 37(8):1715-1731.e11
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EMBO J, 2025, 44(4):1107-1130
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| S7437 |
Sal003
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Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
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Front Pharmacol, 2023, 14:1095307
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bioRxiv, 2023, 2023.05.19.540602
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bioRxiv, 2023, 2023.05.19.540602
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| S7428 |
Rocaglamide
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Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. This compound inhibits the function of the translation initiation factor eIF4A. It also inhibits NF-κB activity. This chemical exhibits anti-tumor activity.
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Life Sci Alliance, 2024, 7(9)e202302396
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Elife, 2023, 12e69521
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Blood Adv, 2023, 7(12):2926-2937
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