Membrane Transporters-Ion Channels

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  1. eIF4A inhibitor

    Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis.
  2. Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
  3. eIF4E-eIF4G interaction inhibitor

    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  4. eIF4A3 inhibitor

    eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM).
  5. cell cycle inhibitor

    Briciclib disodium salt is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity.
  6. PERK inhibitor

    ISRIB (trans-isomer) is a potent and selective small molecule inhibitor of PERK signaling (IC50 ~5 nM) that can potently reverse the effects of eIF2α phosphorylation.
  7. eIF4E/eIF4G inhibitor

    4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 uM.
  8. eIF4F subunit interaction inhibitor

    4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction.
  9. PERK inhibitor

    ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.
  10. Apoptosis inducer

    Episilvestrol is a derivative of Silvestrol, which can induce apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7; 5'myc-UTR-LUC inhibtior (IC50= 0.8 nM).
  11. 4EBP1 inhibitor

    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  12. eIF4A3 inhibitor

    eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM.
  13. GCN2 inhibitor

    GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
  14. GCN2 inhibitor

    GCN2-IN-1 (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
  15. eIF4G1 inhibitor

    SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.
  16. Briciclib, also known as ON 013105 or ON 014185, is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity.
  17. Silvestrol aglycone enantiomer is a cyclopenta benzofuran core phenol.

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