eIF4E/eIF4G PPI-IN-1
eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice.
For research use only. We do not sell to patients.
- Formula: C20H13Cl2N3O2S
- Molecular Weight:430.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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eIF4E 20.2 μM (Kd) |
eIF4G |
Bcl-2 |
eIF4E/eIF4G PPI-IN-1 (Compound A37) (25 μM) shows inhibitory activity against cancer cell lines A549, Hela, HepG2 and MCF-7, with inhibition rates of 98.08, 81.74, 100.78, 78.52%, respectively[1].
eIF4E/eIF4G PPI-IN-1 inhibits the proliferation of A549, Hela, HepG2, and MCF-7 cancer cells, with IC50 values of 4.59 μM, 2.69 μM, 2.22 μM, and 3.45 μM, respectively[1].
eIF4E/eIF4G PPI-IN-1 displays lower cytotoxicity (IC50 > 40 μM) in HEK-293T cells[1].
eIF4E/eIF4G PPI-IN-1 (1-5 μM, 48 h) induces cancer cell apoptosis by regulating the expression of Bcl-2, Bax and C-Caspase-3 proteins in HepG2 cell[1].
eIF4E/eIF4G PPI-IN-1 (2.5 μM, 12 h, 24 h) suppresses HepG2 cell migration[1].
eIF4E/eIF4G PPI-IN-1 (1-5 μM, 48 h) does not induce significant cell cycle arrest in HepG2 cell[1].
eIF4E/eIF4G PPI-IN-1 (1-5 μM, 48 h) plays an anti-tumor effect by inhibiting the expression of Ras, p-MNK, p-ERK and p-eIF4E in HepG2 cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cell
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Concentration:1 μM, 2.5 μM, 5 μM
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Incubation Time:48 h
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Result:Induced 49 % apoptosis of HepG2 cells at 2.5 μM.
Induced HepG2 cells apoptosis over 74 % at 5.0 μM.
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Cell Line:HepG2 cell
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Concentration:2.5 μM
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Incubation Time:12 h, 24 h
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Result:Suppressed HepG2 cell migration.
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Cell Line:HepG2 cell
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Concentration:1 μM, 2.5 μM, 5 μM
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Incubation Time:48 h
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Result:Did not induce significant cell cycle arrest, but increased the G0/G1 phase population at 5 μM.
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Cell Line:HepG2 cell
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Concentration:1 μM, 2.5 μM, 5 μM
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Incubation Time:48 h
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Result:Down-regulated the expression of anti-apoptotic protein Bcl-2 and up-regulated the expression of pro-apoptotic genes Bax and C-Caspase-3.
Inhibited the expression of Ras, p-MNK, p-ERK and p-eIF4E.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2(1 × 107, s.c.) xenograft tumor on the seven-week-old female Balb/c nude mice weighing 16-19 g. mice model[1]
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Dosage:25 mg/kg, 50 mg/kg
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Administration:i.p., once a day, 18 days
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Result:Reduced tumor growth, did not change weight and the shape of organ tissues.
Chemical Information
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Molecular Weight 430.31
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Formula C20H13Cl2N3O2S
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SMILES
OC1=CC=C(C=C1)C2=CC=C(O2)/C=N/NC3=NC(C4=CC(Cl)=C(C=C4)Cl)=CS3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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