Eukaryotic initiation factors (eIFs) are proteins involved in the initiation phase of eukaryotic translation. These proteins help stabilize the formation of the functional ribosome around the start codon and also provide regulatory mechanisms in translation initiation.Eukaryotic initiation factor 2B (eIF2B) is a guanine nucleotide-exchange factor which mediates the exchange of GDP (bound to initiation factor eIF2) for GTP, thus regenerating the active [eIF2.GTP] complex that is required for peptide-chain initiation. The activity of eIF2B is a key control point for eukaryotic protein synthesis and is altered in response to viral infection, hormones, nutrients, growth factors and certain stresses.Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis on capped mRNAs in the cytoplasm. Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factor complex elF4F, which mediates the binding of mRNA to the ribosome.
||4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
||Briciclib is a water soluble derivative of ON 013100, and has the potential in targeting eIF4E for solid cancers.
||SBI-0640756（SBI-756） is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
||4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ∼4 μM.
||eFT226 is a novel, potent and selective eIF4A inhibitor with anti-tumor activity in B-cell malignancies, promotes eIF4A binding to specific mRNA sequences and interferes with the assembly of the eIF4F initiation complex.
||Hippuristanol is a potent, steroid inhibitor of eukaryotic initiation factor 4A (eIF4A), results in cell cycle arrest at G1 phase, and induces caspases activation and apoptosis.
||Elatol (NSC 341593) is a specific inhibitor of ATP hydrolysis by eIF4A1 in vitro with broad activity against multiple tumor types.
||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.
||eIF4A3 inhibitor 53a
||eIF4A3 inhibitor 53a is a potent, selective and cell-active eukaryotic initiation factor 4A3 (eIF4A3) inhibitor with IC50 of 0.26 uM, SPR Kd of 43 nM.
||Metarrestin (ML246) is a specific inhibitor of perinuclear compartment (PNC), disrupts PNCs in PC3M-GFP-PTB cells with IC50 of 0.39 uM, specifically binds eEF1A2.
||Pateamine A (Pateamine) is a potent small molecule inhibitor of eukaryotic translation that stimulates eIF4AI/II and eIF4AIII activity, but not eIF4E, eIF2α, and elF4B.
||A potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM