eif

Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.

eIF4A3-IN-1 is a selective and potent inhibitor of eukaryotic initiation factor 4A3 (eIF4A3) with an IC50 value of 0.26 μM. eIF4A3-IN-1 inhibits cytosolic nonsense-mediated RNA decay at high concentrations.

eIF4A3-IN-2 is a highly selective and noncompetitive inhibitor of eukaryotic initiation factor 4A-3, exhibiting an IC50 of 110 nM.

eIF4A3-IN-5 is a highly effective inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4AI and eIF4AII. With its potent inhibitory properties, eIF4A3-IN-5 shows great potential for advancing research in eIF4A-dependent diseases, including cancer studies.

eIF4A3-IN-7 is a highly effective inhibitor of eIF4A3, exhibiting significant potential for research in cancer and dysproliferative diseases.

eIF4E-IN-3 is a small-molecule inhibitor targeting eIF4E that disrupts cap-dependent mRNA translation initiation. By inhibiting eIF4E function, eIF4E-IN-3 modulates translation of specific proteins and has potential applications in mechanistic studies of eIF4E-dependent diseases such as cancer.

eIF4E-IN-1 (WO2021003194A1, compound Y), is a highly effective inhibitor of eIF4E, a key protein involved in immunosuppression. By targeting immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO, eIF4E-IN-1 functions to disrupt immune suppression and promote immune release in specific diseases such as cancer and infectious diseases.

eIF4E-IN-2 is a highly effective inhibitor of eukaryotic initiation factor 4e (eIF4e). This compound exhibits significant potential in the investigation of eIF4e dependent diseases, particularly in the context of cancer research.

eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.

eIF4E/eIF4G PPI-IN-1 is an inhibitor that disrupts the interaction between eIF4E and eIF4G, exhibiting a dissociation constant (KD) of 20.2 μM for the eIF4E protein. It demonstrates antitumor effects through various mechanisms, including modulation of eIF4E activity via inhibition of the Ras/MAPK/eIF4E signaling pathway, influencing apoptosis and cell migration. Additionally, eIF4E/eIF4G PPI-IN-1 inhibits the growth of HepG2 xenografted tumors in nude mice and is relatively non-toxic to mice.

eIF4A-IN-3 (Compound 71E) is an inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). This compound can be utilized as a cytotoxic payload for antibody-drug conjugates (ADCs).

eIF4A-IN-1 is an eIF4A inhibitor used in tumor research.

eIF4A-IN-2 (Compound 93) is an inhibitor of the eukaryotic translation initiation factor 4A (eIF4A). It serves as a cytotoxic payload in antibody-drug conjugates (ADCs).

eIF3e-IN-1 (Compound 209) is an inhibitor of eIF3e with an EC50 of 18.3 μM. It effectively reduces hypoxia-induced accumulation of the HIF1α protein, thereby inhibiting the acute translational response to hypoxia. Additionally, eIF3e-IN-1 significantly suppresses ATF4 protein expression. This compound is applicable in cancer research, including studies on breast cancer.

eIF4A3-IN-4 is a novel inhibitor of eIF4A with an IC50 of 8.6 μM.

EIF2α activator 2 (Compound 1) is an activator of eIF2α phosphorylation, exhibiting anti-proliferative activity at the μM level in SRB, K562, and PBMC cells, suitable for cancer research.

eIF4A3-IN-6 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A) [e.g., eIF4AI and eIF4AII] with potential for investigation in eIF4A-dependent diseases, including cancer.

(R)-eIF4A3-IN-2, a less active enantiomer of eIF4A3-IN-2, is a highly selective and noncompetitive inhibitor of the eukaryotic initiation factor 4A-3 (eIF4A3) with an IC50 of 110 nM.

eIF4A3-IN-17, a silvestrol analogue, disrupts the assembly of the eIF4F translation complex, exhibiting EC50 values of 0.9, 15, and 1.8 nM for myc-LUC, tub-LUC, and growth inhibition of MBA-MB-231 cells, respectively. This compound holds potential for research in human cancer pathogenesis [1].

eIF4A3-IN-18, a silvestrol analogue, disrupts the formation of the eIF4F translation complex, exhibiting EC 50 values of 0.8, 35, and 2 nM for myc-LUC, tub-LUC, and the growth inhibition of MBA-MB-231 cells, respectively. Additionally, it demonstrates cytotoxicity towards RMPI-8226 cells with an LC 50 of 0.06 nM. This compound is utilized in researching human cancer pathogenesis [1].

eIF4A3-IN-9, a silvestrol analogue, disrupts the assembly of the eIF4F translation complex, exhibiting EC50 values of 29, 450, and 80 nM for myc-LUC, tub-LUC, and growth inhibition in MBA-MB-231 cells, respectively. It is utilized in researching human cancer pathogenesis [1].

eIF4E-IN-5 (Compound 6n) is a cell-permeable inhibitor of eIF4E that binds to capped mRNA, inhibiting cap-dependent translation [1].

eIF4E-IN-6 (Compound 4b), a GMP analog, is designed to inhibit the eIF4E protein's ability to bind to cap mRNA. It demonstrates cytotoxic effects on Caco-2, HepG-2, and MCF-7 cell lines with IC50 values of 31, 27, and 21 μM, respectively [1].

eIF4A i28, an inhibitor of the eukaryotic initiation factor-4A (eIF4A) with an IC50 of 8.60 μM in an eIF4A ATPase assay, effectively reduces the viability of BJAB Burkitt lymphoma cells, as indicated by an EC50 of 0.46 μM in a CellTiter-Glo (CTG) luminescence cell viability assay. This compound functions as an RNA-competitive, ATP-uncompetitive eIF4A inhibitor.