S2923 |
Salubrinal
|
Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay. |
-
Cell Death Dis, 2024, 15(1):31
-
Respir Res, 2024, 25(1):201
-
Cell Genom, 2024, 4(2):100487
|
|
S7369 |
4EGI-1
|
4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis. |
-
Nat Commun, 2024, 15(1):4083
-
Nat Commun, 2024, 15(1):4083
-
Nucleic Acids Res, 2024, gkae849
|
|
S0706 |
ISRIB
|
ISRIB is an integrated stress response (ISR) inhibitor that potently reverses the effects of eukaryotic initiation factor 2α (eIF2α) phosphorylation. |
-
Nat Commun, 2024, 15(1):546
-
Exp Mol Med, 2024, 56(2):408-421.
-
Cell Rep, 2024, 43(7):114487
|
|
S8275 |
Tomivosertib (eFT-508)
|
Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance. |
-
J Clin Invest, 2024, 134(16)e168393
-
Sci Adv, 2024, 10(37):eadi7673
-
PLoS Biol, 2023, 21(8):e3002227
|
|
S7370 |
4E1RCat
|
4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E. |
-
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
-
Cell Chem Biol, 2021, S2451-9456(21)00213-0
-
J Cell Mol Med, 2021, 10.1111/jcmm.16307
|
|
S7437 |
Sal003
|
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
-
Front Pharmacol, 2023, 14:1095307
-
bioRxiv, 2023, 2023.05.19.540602
-
bioRxiv, 2023, 2023.05.19.540602
|
|
S7428 |
Rocaglamide
|
Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity. |
-
Life Sci Alliance, 2024, 7(9)e202302396
-
Elife, 2023, 12e69521
-
Blood Adv, 2023, 7(12):2926-2937
|
|
S9668 |
PKR-IN-C16
|
PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. |
-
Exp Mol Med, 2024, 56(2):408-421.
-
EMBO J, 2024, 43(5):780-805.
-
Respir Res, 2024, 25(1):201
|
|
S8181 |
SBI-0640756
|
SBI-0640756(SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex. It can also suppress AKT and NF-κB signaling. |
-
Sci Rep, 2021, 11(1):21689
|
|
E4888New |
Guanabenz hydrochloride
|
Guanabenz hydrochloride(NE56490) is a small molecule, antihypertensive agonist of α2-adrenoceptor. It also inhibits eIF2α and GADD34, showing potential for treating cardiac hypertrophy, heart failure, atherosclerosis, and ischemic heart disease. |
|
|
S6533 |
Briciclib
|
Briciclib (ON-014185) is a water soluble derivative of ON-013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E). |
|
|
S8994New |
Zotatifin
|
Zotatifin (eFT226) is a highly effective and sequence-selective inhibitor of the RNA helicase eIF4A. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5'-UTRs, with an IC50 of 2 nM, and disrupts the assembly of the eIF4F initiation complex. By enhancing the interaction between eIF4A and polypurine RNA sequence or structural motifs, zotatifin converts eIF4A into a sequence-specific translation repressor, thereby regulating the translation of certain target genes. It also exhibits anti-tumor activity. |
|
|
S2961 |
GC7 Sulfate
|
GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins. |
-
Exp Mol Med, 2024, 10.1038/s12276-024-01214-1
|
|
S2923 |
Salubrinal
|
Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay. |
- Cell Death Dis, 2024, 15(1):31
- Respir Res, 2024, 25(1):201
- Cell Genom, 2024, 4(2):100487
|
|
S7369 |
4EGI-1
|
4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis. |
- Nat Commun, 2024, 15(1):4083
- Nat Commun, 2024, 15(1):4083
- Nucleic Acids Res, 2024, gkae849
|
|
S0706 |
ISRIB
|
ISRIB is an integrated stress response (ISR) inhibitor that potently reverses the effects of eukaryotic initiation factor 2α (eIF2α) phosphorylation. |
- Nat Commun, 2024, 15(1):546
- Exp Mol Med, 2024, 56(2):408-421.
- Cell Rep, 2024, 43(7):114487
|
|
S8275 |
Tomivosertib (eFT-508)
|
Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance. |
- J Clin Invest, 2024, 134(16)e168393
- Sci Adv, 2024, 10(37):eadi7673
- PLoS Biol, 2023, 21(8):e3002227
|
|
S7370 |
4E1RCat
|
4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E. |
- Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
- Cell Chem Biol, 2021, S2451-9456(21)00213-0
- J Cell Mol Med, 2021, 10.1111/jcmm.16307
|
|
S7437 |
Sal003
|
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
- Front Pharmacol, 2023, 14:1095307
- bioRxiv, 2023, 2023.05.19.540602
- bioRxiv, 2023, 2023.05.19.540602
|
|
S7428 |
Rocaglamide
|
Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity. |
- Life Sci Alliance, 2024, 7(9)e202302396
- Elife, 2023, 12e69521
- Blood Adv, 2023, 7(12):2926-2937
|
|
S9668 |
PKR-IN-C16
|
PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. |
- Exp Mol Med, 2024, 56(2):408-421.
- EMBO J, 2024, 43(5):780-805.
- Respir Res, 2024, 25(1):201
|
|
S8181 |
SBI-0640756
|
SBI-0640756(SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex. It can also suppress AKT and NF-κB signaling. |
- Sci Rep, 2021, 11(1):21689
|
|
E4888New |
Guanabenz hydrochloride
|
Guanabenz hydrochloride(NE56490) is a small molecule, antihypertensive agonist of α2-adrenoceptor. It also inhibits eIF2α and GADD34, showing potential for treating cardiac hypertrophy, heart failure, atherosclerosis, and ischemic heart disease. |
|
|
S6533 |
Briciclib
|
Briciclib (ON-014185) is a water soluble derivative of ON-013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E). |
|
|
S8994New |
Zotatifin
|
Zotatifin (eFT226) is a highly effective and sequence-selective inhibitor of the RNA helicase eIF4A. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5'-UTRs, with an IC50 of 2 nM, and disrupts the assembly of the eIF4F initiation complex. By enhancing the interaction between eIF4A and polypurine RNA sequence or structural motifs, zotatifin converts eIF4A into a sequence-specific translation repressor, thereby regulating the translation of certain target genes. It also exhibits anti-tumor activity. |
|
|
S2961 |
GC7 Sulfate
|
GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins. |
- Exp Mol Med, 2024, 10.1038/s12276-024-01214-1
|
|