Eukaryotic Initiation Factor (eIF)

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  1. eIF4F Inhibitor

    eIF4A3-IN-13 is an inhibitor of the eIF4F translation complex, functioning through disruption of its assembly. This compound exhibits potent biological activity, with EC50 values of 0.6 nM for myc-LUC, 15 nM for tub-LUC, and 0.4 nM for growth inhibition in MBA-MB-231 breast cancer cells. eIF4A3-IN-13 is a valuable tool for investigating the mechanisms of human cancer pathogenesis and exploring therapeutic strategies targeting translation regulation.
  2. eIF4F Inhibitor

    eIF4A3-IN-11 is a potent inhibitor of the eIF4F translation complex. It effectively disrupts complex assembly, exhibiting EC50 values of 0.2 nM for myc-Luciferase, 4 nM for tubulin-Luciferase, and 0.3 nM for the inhibition of MBA-MB-231 cancer cell growth. This compound is valuable for investigating the molecular mechanisms underlying human cancer pathogenesis.
  3. eIF4A Inhibitor

    eIF4A3-IN-14 is a selective inhibitor of eIF4A, a crucial component of the eIF4F translation complex. This compound demonstrates potent inhibitory activity with an EC50 of approximately 40 nM against myc-LUC and over 2000 nM against tub-LUC. eIF4A3-IN-14 is valuable for investigating tumorigenesis and the molecular mechanisms of translational regulation in cancer research.
  4. eIF Inhibitor

    CMLD012612 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), designed to disrupt the translation initiation process in eukaryotic cells. This amidino-rocaglate compound features a hydroxamate group, demonstrating significant cytotoxicity in NIH/3T3 cells, with an IC50 value of 2 nM. By modifying the activity of the RNA helicase eIF4A, CMLD012612 exhibits promising anti-neoplastic properties, making it a valuable tool for cancer research and studies focused on translation regulation.
  5. EIF2b Activator

    Fosigotifator is an orally active activator of eukaryotic initiation factor 2B (eIF2B), known for its ability to penetrate the blood-brain barrier. By stabilizing the eIF2B complex, Fosigotifator enhances its activity, particularly in the context of pathogenic vanishing white matter (VWM) mutations. As an integrated stress response inhibitor (ISRI), this compound is valuable for research in neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS).
  6. eIF Inhibitor

    CMLD012073 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), functioning through the mechanism of amidino-rocaglates. This compound effectively inhibits cell growth in NIH/3T3 cells with an IC50 value of 10 nM. CMLD012073 disrupts eukaryotic translation initiation by altering the activity of the RNA helicase eIF4A, making it a valuable tool for research applications related to protein synthesis and gene regulation.
  7. eIF Inhibitor

    CMLD012072 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4A1 and eIF4A2 through RNA clamping. This amidino-rocaglate compound exhibits significant anti-neoplastic activity, making it a valuable tool for researching the role of eIF4A in cancer biology and therapeutic interventions. Its mechanism of action provides insight into the regulation of protein synthesis in neoplastic cells, facilitating further studies in oncology and molecular biology.
  8. eIF4A3 Inhibitor

    eIF4A3-IN-7 is a potent inhibitor of the eIF4A3 protein, a key regulator of mRNA translation and splicing. This compound demonstrates significant potential for research in cancer and other dysproliferative diseases by modulating gene expression pathways. Its targeted mechanism of action may provide valuable insights into the role of eIF4A3 in tumorigenesis and other pathological conditions.
  9. eIF2α Activator

    1,3-Bis[3,5-bis(trifluoromethyl)phenyl]urea is a potent activator of the eIF2α kinase heme-regulated inhibitor. It effectively reduces the levels of the eIF2·GTP·tRNAiMet ternary complex, thereby modulating protein synthesis. This compound also demonstrates significant inhibitory effects on cancer cell proliferation, making it a valuable tool in cancer research and investigations into cellular stress responses.
  10. eIF4E Inhibitor

    eIF4E-IN-1 is a potent inhibitor of the eIF4E protein, which plays a critical role in regulating protein synthesis and cell proliferation. This compound effectively targets and inhibits immunosuppressive components, including immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO. eIF4E-IN-1 demonstrates promising biological activity in the modulation of immune responses, making it a valuable tool for research applications in cancer and infectious disease therapies.
  11. Integrated Stress Response Modulator

    PRXS571 is a potent modulator of the integrated stress response (ISR) in neurons. This compound enhances our understanding of the cellular mechanisms underlying stress adaptation, making it valuable for research into neurodegenerative diseases and other neurological conditions. PRXS571 can be utilized to investigate the role of ISR modulation in various biological processes and therapeutic applications.
  12. GCN2-targeting Agent

    RAPT-37-Me is a selective GCN2 inhibitor that demonstrates potent activity with an IC50 of 0.002 μM for GCN2, alongside higher IC50 values of more than 10 μM for PERK, 4.40 μM for HRl, and 1.31 μM for PKR. This compound is valuable for research applications focused on the integrated stress response and its implications in various diseases, offering insights into GCN2-mediated signaling pathways. It is particularly relevant for studies investigating therapeutic interventions that modulate cellular stress responses.
  13. ISR Modulator

    ISR Modulator-1 is a compound that targets the integrated stress response (ISR) pathway. It functions by modulating cellular responses to stressors, enhancing cell survival under adverse conditions. This reagent is valuable for research applications investigating the mechanisms of cellular stress, neurodegenerative diseases, and metabolic disorders.
  14. MNK1/MNK2 Inhibitor

    HD202A is a selective dual inhibitor of MNK1 and MNK2, exhibiting IC50 values of 6.09 nM and 8.06 nM, respectively. This compound effectively inhibits the MNK-eIF4E signaling pathway, leading to downregulation of perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α. HD202A enhances mitochondrial fatty acid oxidation, redox homeostasis, and demonstrates significant effects on metabolic health, including suppression of body weight gain, reduction in hepatic lipid accumulation, and improvement in glucose tolerance and insulin sensitivity. These properties make HD202A a valuable tool for researching metabolic dysfunction-associated steatotic liver disease.
  15. eIF4A Inhibitor

    eIF4A-IN-1 is a selective inhibitor of eIF4A, a key protein involved in the regulation of mRNA translation. This compound effectively reduces protein synthesis in cancer cells by disrupting the initiation of translation, thereby providing a valuable tool for investigating tumor biology. eIF4A-IN-1 is applicable in studies focused on cancer therapeutics and understanding the mechanisms of tumorigenesis.
  16. eIF4A Inhibitor

    eIF4A3-IN-5 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4AI and eIF4AII. This compound demonstrates significant potential for investigating eIF4A-dependent diseases, particularly in the context of cancer research. Its ability to modulate eIF4A activity makes it a valuable tool for studying mechanisms of protein synthesis and their implications in tumorigenesis.
  17. ISR Activator

    ISR Activator 3 (Compound cc81) is a potent activator of the integrated stress response (ISR), targeting RIG-I with a dissociation constant of approximately 0.55 μM. This compound enhances the interferon response in the presence of viral mimicry signals while not inducing lipid droplet clearance. ISR Activator 3 is suitable for research related to neurodegenerative diseases and immune stress mechanisms, providing valuable insights into cellular stress pathways and their implications in various biological contexts.
  18. Promoter

    NVS2.1 is a potent, orally bioavailable readthrough promoter that targets ribosome-associated quality control mechanisms. By promoting the degradation of eRF1, NVS2.1 activates pathways involving GCN1, RNF14, and RNF25, enabling the translation process to bypass premature termination codons. This compound is valuable for research focused on genetic disorders resulting from nonsense mutations.
  19. eIF4E Inhibitor

    eIF4E-IN-4 is a selective inhibitor of eukaryotic initiation factor 4E (eIF4E), demonstrating a biochemical activity value of 95 nM. This compound effectively inhibits cap-dependent mRNA translation, exhibiting an IC50 value of 2.5 μM. eIF4E-IN-4 is valuable for research applications related to breast cancer, colon cancer, and head and neck cancer, providing insights into the role of eIF4E in malignancies.
  20. eIF4A Inhibitor

    eIF4A3-IN-6 is a selective inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4AI and eIF4AII. This compound exhibits significant biological activity in disrupting eIF4A-mediated processes, making it a valuable tool for studying eIF4A-dependent diseases, particularly in cancer research. The potential applications of eIF4A3-IN-6 extend to elucidating the role of eIF4A in oncogenic mechanisms and therapeutic interventions.
  21. GCN2-targeting Agent

    AMG-34 is a selective GCN2-targeting agent that exhibits an IC50 of 0.395 μM for GCN2, along with IC50 values of 0.010 μM for PERK, 1.07 μM for HR and PKR, and greater than 10 μM for other targets. This compound is instrumental in research focused on the cellular stress response and the role of GCN2 in regulating protein synthesis. Its inhibitory activity makes it a valuable tool for studies exploring the therapeutic potential of modulating the integrated stress response.
  22. MNK1/2 Inhibitor

    MNK1/2-IN-7 is a selective inhibitor of MNK1 and MNK2, primarily targeting the MNK/eIF4E signaling pathway. This compound exhibits potent anticancer activity by effectively inhibiting the phosphorylation of eIF4E, which contributes to reduced cancer cell proliferation. Additionally, MNK1/2-IN-7 demonstrates favorable hERG safety profiles, making it a valuable tool for research applications in oncology, particularly in combination therapies with agents like Ibrutinib.
  23. eIF4A Inhibitor

    Zotatifin is a highly selective inhibitor of eIF4A, targeting the assembly of the eIF4F initiation complex. With an IC50 of 2 nM, it promotes eIF4A binding to specific mRNA recognition motifs in the 5’-UTRs. Zotatifin exhibits significant antiviral properties, effectively reducing the infectivity of SARS-CoV-2 by inhibiting the biogenesis of its NP protein (IC90 = 37 nM) and also induces apoptosis in cancer cells. This compound is valuable for studies related to viral infections and translational control mechanisms.
  24. eIF4G1 Inhibitor

    SBI-0640726 is an eIF4G1 inhibitor that exerts antiproliferative effects in melanoma. It disrupts the eIF4F translation initiation complex by targeting the AKT and NF-kB signaling pathways. This compound has demonstrated the ability to inhibit the growth of NRAS and BRAF mutant melanoma cells in vitro, making it a valuable tool for research in cancer biology and therapeutic development.
  25. eIF4A Inhibitor

    rel-Zotatifin is a racemic isomer of Zotatifin, functioning as an inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound exhibits biological activity by promoting eIF4A binding to specific mRNA sequences in the 5’-UTRs, thereby disrupting the assembly of the eIF4F initiation complex. Its key research applications include the study of translation regulation and potential therapeutic interventions in conditions driven by aberrant protein synthesis.
  26. eIF4E-eIF4G interaction inhibitor

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

    eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM).
  28. 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.
  29. 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.
  30. 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.
  31. PERK inhibitor

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

  32. eIF4F subunit interaction inhibitor

    4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction.
  33. eIF2α phosphatase inhibitor

    Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
  34. 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).
  35. Silvestrol aglycone enantiomer is a cyclopenta benzofuran core phenol.
  36. eIF4G1 inhibitor

    SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.
  37. 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.
  38. 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.
  39. 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.
  40. EIF2AK3/PERK activator

    CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
  41. eIF4A3 inhibitor

    eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM.
  42. 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).
  43. eIF4A Inhibitor

    Didesmethylrocaglamide is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), a key player in the regulation of protein synthesis. This compound demonstrates significant growth-inhibitory activity with an IC50 of 5 nM, effectively suppressing various growth-promoting signaling pathways and inducing apoptosis in tumor cells. Didesmethylrocaglamide is primarily utilized in cancer research to explore its potential therapeutic applications in oncology.
  44. eIF4A Inhibitor

    Rohinitib is a selective inhibitor of eIF4A, a critical protein involved in the regulation of translation initiation. It has demonstrated the ability to induce apoptosis in acute myeloid leukemia (AML) cell lines and effectively reduces leukemia burden in AML xenograft models. Rohinitib is a valuable tool for investigating the mechanisms of AML and exploring potential therapeutic strategies.
  45. eIF4A Inhibitor

    MG-002 is a selective eIF4A inhibitor that interferes with the recruitment and scanning of ribosomes by non-productively trapping the eukaryotic translation initiation factor 4A (eIF4A) onto RNA. This action effectively inhibits mRNA translation, leading to reduced growth and metastasis of triple-negative breast cancer (TNBC) tumors, as well as inducing apoptosis in cancer cells. Additionally, MG-002 significantly downregulates the protein expression of c-MYC and cyclin D1, making it a valuable tool for research applications focused on TNBC and other related malignancies.
  46. eIF4A Inhibitor

    CR-1-31-B is a synthetic rocaglate that serves as a potent inhibitor of the eukaryotic translation initiation factor eIF4A. By disrupting the interaction between eIF4A and RNA, CR-1-31-B impedes the initiation phase of protein synthesis. This compound has been shown to affect the association of Plasmodium falciparum eIF4A with RNA and induce apoptosis in neuroblastoma and gallbladder cancer cells, making it a valuable tool for studying mechanisms of protein synthesis and cancer biology.
  47. eIF4E Inhibitor

    Antiproliferative agent-64 is a potent inhibitor of eukaryotic translation initiation factor 4E (eIF4E), which disrupts the secondary structure of mRNA to effectively inhibit protein translation. This compound exhibits significant biological activity by targeting the 5' untranslated region (5'UTR) of c-Myc with an EC50 of 1.2 nM and the 5'UTR encoding tubulin with an EC50 of 40 nM. Antiproliferative agent-64 also demonstrates considerable antiproliferative effects on MDA-MB-231 cancer cells, with an EC50 of 7 nM, making it a valuable tool for cancer research and the study of translation regulation.

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