Catalog No.
Product Name
Application
Product Information
Citations
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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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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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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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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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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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eIF4G1 inhibitor
SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex. -
eIF4A3 inhibitor
eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM. -
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). -
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. -
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. - 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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
