eIF4A3-IN-18 (compound 74) is a silvestrol (HY-13251) analogue. eIF4A3-IN-18 interferes the assembling of eIF4F translation complex with EC50 values of 0.8, 35 and 2 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-18 also has cytotoxicity to RMPI-8226 cells with an LC50 of 0.06 nM. eIF4A3-IN-18 can be used for the research of human cancer pathogenesis[1].
eIF4A3-IN-13 (compound 75) is a silvestrol (HY-13251) analogue. eIF4A3-IN-13 interferes the assembling of eIF4F translation complex with EC50s of 0.6, 15 and 0.4 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-13 can be used for the research of human cancer pathogenesis[1].
ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A[1].
EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation[1][2].
ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden[1].
GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity[1][2].
CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 against NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A)[1].
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity[1].
eIF4E-IN-3 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-3 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 485)[1].
CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity[1].
eIF4A3-IN-17 (compound 61) is a silvestrol (HY-13251) analogue. eIF4A3-IN-17 interferes the assembling of eIF4F translation complex with EC50s of 0.9, 15 and 1.8 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-17 can be used for the research of human cancer pathogenesis[1].
eIF4A3-IN-12 (compound 62) is a silvestrol (HY-13251) analogue. eIF4A3-IN-12 interferes the assembling of eIF4F translation complex with EC50s of 4, 70 and 5 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-12 can be used for the research of human cancer pathogenesis[1].
eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-2 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 1188)[1].
eIF4A3-IN-16 (compound 60) is a silvestrol (HY-13251) analogue. eIF4A3-IN-16 interferes the assembling of eIF4F translation complex with EC50s of 1, 30 and 1 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-16 can be used for the research of human cancer pathogenesis[1].
eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y)[1].
BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells[1].
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD[1].
DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation[1].
Rohinitib is a potent and specific inhibitor of eIF4A1, inhibits growth and survival of AML cells especially cells with FLT3-ITD.
4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ∼4 μM.
2BAct (eIF2B activator 2BAct) is a novel, highly selective, CNS-permeable small molecule eIF2B activator with EC50 of 33 nM in cell-based reporter assays; 2BAct normalized body weight gain and prevented motor deficits in male R191H mice, prevented myelin loss and reactive gliosis in the brain and spinal cord of R191H mice; also prevented ISR induction in the cerebellum and spinal cord of Eif2b5R132H/R132H mice, prevented all measures of pathology and normalizes the transcriptome and proteome of Vanishing White Matter (VWM) mice.
eIF4A3-IN-7 is a potent inhibitor of eIF4A3. eIF4A3-IN-7 has the potential for researching cancer and other dysproliferative diseases (extracted from patent WO2019161345A1, Compound 8)[1].
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM.
eIF4A3-IN-6 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), such as eIF4AI and eIF4AII. eIF4A3-IN-6 has the potential for the research of eIF4A dependent diseases, including the research of cancer (extracted from patent US20170145026A1)[1].
CCT020312 is capable of delivering potent, and eukaryotic initiation factor 2-alpha kinase 3 (EIF2AK3) selective, proliferation control and also is an activator of RNA-like endoplasmic reticulum kinase (PERK).
eIF4A3-IN-11 (compound 56) is a silvestrol (HY-13251) analogue. eIF4A3-IN-11 interferes the assembling of eIF4F translation complex with EC50s of 0.2, 4 and 0.3 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-11 can be used for the research of human cancer pathogenesis[1].
eIF4A3-IN-10 (compound 58) is a silvestrol (HY-13251) analogue. eIF4A3-IN-10 interferes the assembling of eIF4F translation complex with EC50s of 35 and 100 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-10 can be used for the research of human cancer pathogenesis[1].
eIF4A3-IN-9 (compound 57) is a silvestrol (HY-13251) analogue. eIF4A3-IN-9 interferes the assembling of eIF4F translation complex with EC50s of 29, 450 and 80 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-9 can be used for the research of human cancer pathogenesis[1].