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eEF2K degrader C1 is a small-molecule degrader of eEF2K, acts a molecular glue to enhance the interaction of eEF2K with the ubiquitin E3 ligase βTRCP, thereby promoting the proteasomal degradation of eEF2K.
MG-002 is a second-generation, orally bioavailable inhibitor of eIF4A, a key RNA helicase involved in the initiation of cap-dependent mRNA translation. By targeting eIF4A, MG-002 effectively disrupts the translation of certain mRNAs, particularly those with complex 5' untranslated regions (UTRs) that are highly dependent on eIF4A activity. This mechanism of action makes MG-002 a promising candidate for targeting cancers and other diseases driven by dysregulated translation.
EGPI-1 is a potent small molecule that inhibits the translation initiation factors eIF4E/eIF4G interaction.EGPI-1 has potent antiproliferative and proapoptotic activity in multiple myeloma cells, Jurkat cells, and A549 lung cancer cell lines, inhibts A549 proliferation with IC50 of 2.61 uM, which is better than that of 4EGI-1 (IC50=58.6 uM), inhibits cancer cell growth by inhibiting eIF4E phosphorylation and inhibiting PI3K/Akt/mTOR signal pathway.EGPI-1 induces autophagy, apoptosis, G0/G1 cell cycle arrest and ROS generation in A549 cells, disrupts the mitochondrial membrane potential (∆ψ m).EGPI-1 demonstrated in vivo anti-tumor activities in A549-xenografted athymic mice (25 mg/kg/day, 50 mg/kg/day, i.p.).
Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.
3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research.
SBI-5844 (SBI-1275844) is a small molecule inhibitor of coronaviruses translation initiation complex 4F (eIF4F), disrupts eIF4F complex formation and inhibits coronavirus RNA and protein levels.
SBI-0498 (SBI-0730498) is a small molecule inhibitor of coronaviruses translation initiation complex 4F (eIF4F), disrupts eIF4F complex formation and inhibits coronavirus RNA and protein levels.
eEF2K degrader C1 is a small-molecule degrader of eEF2K, acts a molecular glue to enhance the interaction of eEF2K with the ubiquitin E3 ligase βTRCP, thereby promoting the proteasomal degradation of eEF2K.
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