Catalog No.
Product Name
Application
Product Information
Citations
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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. - 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.
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eIF2α dephosphorylation inhibitor
Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).- Gregory R. Kardos, .et al. , Front Oncol, 2020, 10: 834 PMID: 32637352
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eIF4A3 inhibitor
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM). -
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. -
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.
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eIF4E/eIF4G inhibitor
4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 uM.- Amnon Wittenstein, .et al. , PLoS Biol, 2023, Nov 9;21(11):e3002355 PMID: 37943958
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PERK inhibitor
ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.- Le Xu, .et al. , Cell Stem Cell, 2024, Aug 16:S1934-5909(24)00287-X PMID: 39181129
- SeungHye Han, .et al. , Nature, 2023, Aug;620(7975):890-897 PMID: 37558881
- Zhou W, .et al. , Research Square, 2023, MAY 03
- Satoshi Watanabe, .et al. , Proc Natl Acad Sci U S A, 2021, May 18;118(20) PMID: 33972447
- Satoshi Watanabe, .et al. , bioRxiv, 2020, February 27
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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). -
eIF4A3 inhibitor
eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM. -
eIF4G1 inhibitor
SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex. - Silvestrol aglycone enantiomer is a cyclopenta benzofuran core phenol.
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
eIF4A Inhibitor
eIF4A-IN-2 is a potent inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound demonstrates significant cytotoxic activity and can be utilized as a valuable payload in the synthesis of antibody-drug conjugates (ADCs). Researchers investigating translation regulation and therapeutic strategies in cancer may find eIF4A-IN-2 particularly useful for advancing their studies. -
EIF2α Activator
HR-19011 is an eIF2α phosphorylation activator that specifically targets the heme-regulated inhibitor HRI (EIF2AK1). It demonstrates significant growth inhibitory activity against K562 leukemia cells, with an IC50 value of 3.91 µM. By activating the integrated stress response through the HRI-eIF2α-ATF4 axis, HR-19011 effectively contributes to the suppression of hematologic malignancies. Its favorable safety profile in vivo further supports its use in research focused on leukemia and other blood-related cancers. -
eIF2B Activator
2BAct is a selective activator of the eukaryotic initiation factor 2B (eIF2B) with an EC50 of 33 nM. This compound effectively prevents neurological defects associated with a chronic integrated stress response, making it a valuable tool for research in neurobiology and stress response mechanisms. Additionally, 2BAct demonstrates enhanced solubility and improved pharmacokinetic properties compared to the eIF2B activator ISRIB trans-isomer. -
eIF Inhibitor
GCN2-IN-6 is a selective inhibitor of GCN2, exhibiting potent activity with an IC50 of 1.8 nM in enzymatic assays and 9.3 nM in cellular contexts. Additionally, this compound acts as an eIF2α kinase PERK inhibitor, demonstrating an IC50 of 0.26 nM enzymatically and 230 nM in cellular assays. GCN2-IN-6 also features an alkyne functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it valuable for biochemical research applications. -
eIF4e Inhibitor
eIF4E-IN-2 is a potent inhibitor targeting eukaryotic initiation factor 4E (eIF4E), with an IC50 of 13 nM. This compound effectively inhibits the proliferation of MDA-MB-361 breast cancer cells, thereby demonstrating its potential in cancer research. eIF4E-IN-2 can be utilized for studies investigating the role of eIF4E in breast cancer progression and therapeutic interventions. -
EIF2α Activator
EIF2α Activator 2 is a potent activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. It demonstrates significant antiproliferative activity, with IC50 values of 4.79 μM against K562 cells and 10.52 μM against peripheral blood mononuclear cells (PBMCs). This compound is primarily used in research focused on understanding the regulatory mechanisms of protein synthesis and cell proliferation. -
eIF4A3 Inhibitor
eIF4A3-IN-8 is a selective ATP-competitive inhibitor targeting eukaryotic initiation factor 4A3 (eIF4A3). This compound functions as a valuable chemical probe for investigating the role of eIF4A3 in mRNA processing and the exon junction complex (EJC). Its ability to modulate eIF4A3 activity makes it a useful tool for research into gene expression regulation and related biological pathways. -
eIF4E/eIF4G Interaction Inhibitor
(Z)-4EGI-1 is an inhibitor of the interaction between eIF4E and eIF4G, targeting translation initiation. With an IC50 of 43.5 μM and a Kd value of 8.74 μM, (Z)-4EGI-1 demonstrates significant binding affinity for eIF4E. This compound exhibits anticancer activity, making it a valuable tool for research in cancer biology and studies focused on the regulation of protein synthesis. -
eIF4F Inhibitor
eIF4A3-IN-18 is an effective eIF4F inhibitor that disrupts the assembly of the eIF4F translation complex. It demonstrates potent biological activity with EC50 values of 0.8 nM for myc-LUC, 35 nM for tub-LUC, and inhibits growth in MBA-MB-231 cells. Additionally, eIF4A3-IN-18 exhibits significant cytotoxicity towards RMPI-8226 cells, with an LC50 of 0.06 nM. This compound is valuable for research into the mechanisms of human cancer pathogenesis. -
eIF4F Inhibitor
eIF4A3-IN-12 is an eIF4F inhibitor, specifically disrupting the assembly of the eIF4F translation complex. With EC50 values of 4 nM for myc-LUC, 70 nM for tub-LUC, and 5 nM for inhibiting the growth of MBA-MB-231 cells, this compound demonstrates potent biological activity. eIF4A3-IN-12 is valuable for investigating human cancer pathogenesis and understanding the role of translation regulation in tumorigenesis. -
eIF4A3-IN-2 Less Active Enantiomer
(R)-eIF4A3-IN-2 is the less active enantiomer of eIF4A3-IN-2, a selective noncompetitive inhibitor of eukaryotic initiation factor 4A-3 (eIF4A3). With an IC50 of 110 nM, eIF4A3-IN-2 demonstrates significant inhibition of eIF4A3, impacting mRNA splicing and translation processes. This compound is useful in research applications focused on cancer biology, novel therapeutic pathways, and the regulation of gene expression. -
eIF4F Inhibitor
eIF4A3-IN-16 is a potent eIF4F inhibitor that selectively disrupts the assembly of the eIF4F translation complex. It demonstrates significant biological activity, inhibiting MBA-MB-231 cell growth with an EC50 of 1 nM. Additionally, eIF4A3-IN-16 affects myc-LUC and tub-LUC with EC50 values of 1 nM and 30 nM, respectively. This compound is applicable in research focused on triple negative breast cancer (TNBC). -
EIF2b Activator
Fosigotifator THAM sodium is a potent activator of eukaryotic initiation factor 2B (EIF2B), enhancing its stability and function. This compound is capable of penetrating the blood-brain barrier and demonstrates efficacy in boosting EIF2B activity, particularly in scenarios involving pathogenic vanishing white matter (VWM) mutations. As an integrated stress response inhibitor, Fosigotifator THAM sodium serves as a valuable tool in research focused on amyotrophic lateral sclerosis and related neurodegenerative conditions. -
eIF4e Inhibitor
eIF4E-IN-3 is a highly effective inhibitor of eukaryotic initiation factor 4E (eIF4E), a critical component in the protein synthesis initiation pathway. This compound demonstrates significant potential in investigating eIF4E-dependent diseases, particularly in cancer research. By modulating eIF4E activity, eIF4E-IN-3 offers valuable insights into the molecular mechanisms underlying tumorigenesis and may aid in the development of targeted therapeutic strategies. -
eIF4F Inhibitor
eIF4A3-IN-15 is a targeted inhibitor of the eIF4F translation complex, effectively disrupting its assembly. This compound demonstrates potent activity with EC50 values of 11, 700, and 120 nM against myc-LUC and tub-LUC, as well as growth inhibition in MBA-MB-231 cancer cells. eIF4A3-IN-15 is suitable for research applications focused on understanding the mechanisms underlying human cancer pathogenesis. -
eIF4F Inhibitor
eIF4A3-IN-9 is a potent eIF4F inhibitor that disrupts the formation of the eIF4F translation complex. Demonstrating EC50 values of 29 nM for myc-LUC, 450 nM for tub-LUC, and an effective growth inhibition in MBA-MB-231 cells, this compound serves as a valuable tool in the study of cancer biology. Its targeted action makes it suitable for investigating human cancer pathogenesis and exploring therapeutic strategies against malignancies. -
eIF Inhibitor
eIF4A3-IN-4 is a selective inhibitor of the eIF4A protein, exhibiting an IC50 value of 8.6 μM. This compound is relevant for research applications targeting the regulation of translation initiation and the modulation of gene expression. It has potential utility in studying cancer biology and other disorders related to abnormal protein synthesis. -
eIF4F Inhibitor
eIF4A3-IN-10 is an inhibitor of the eIF4F translation complex. It exhibits significant biological activity, with EC50 values of 35 nM for myc-LUC and 100 nM for growth inhibition in MBA-MB-231 cancer cells. This compound serves as a valuable tool in researching the pathogenesis of human cancers, particularly in the context of disrupted translation regulation associated with tumorigenesis. -
eIF4F Inhibitor
eIF4A3-IN-17 is an eIF4F inhibitor that disrupts the assembly of the eIF4F translation complex. It has demonstrated potent biological activity with EC50 values of 0.9 nM for myc-LUC, 15 nM for tub-LUC, and 1.8 nM for inhibiting the growth of MBA-MB-231 cells. This compound can be utilized in research focused on understanding human cancer pathogenesis and the mechanisms underlying oncogenic translation regulation. -
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. -
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. -
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.
