2. Cell Cycle/DNA Damage Apoptosis MAPK/ERK Pathway GPCR/G Protein
  3. Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Ras PERK
  4. 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.

eIF4E/eIF4G PPI-IN-1 Chemical Structure

eIF4E/eIF4G PPI-IN-1 Chemical Structure

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eIF4E/eIF4G PPI-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

eIF4E

20.2 μM (Kd)

eIF4G

 

Bcl-2

 

In Vitro

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 for A549, Hela, HepG2, and MCF-7, 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) 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.

eIF4E/eIF4G PPI-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HepG2 cell
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Induced 49 % apoptosis of HepG2 cells at 2.5 μM.
Induced HepG2 cells apoptosis over 74 % at 5.0 μM.

Cell Migration Assay [1]

Cell Line: HepG2 cell
Concentration: 2.5 μM
Incubation Time: 12 h, 24 h
Result: Suppressed HepG2 cell migration.

Cell Cycle Analysis[1]

Cell Line: HepG2 cell
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Did not induce significant cell cycle arrest, but increased the G0/G1 phase population at 5 μM.

Western Blot Analysis[1]

Cell Line: HepG2 cell
Concentration: 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
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.
In Vivo

eIF4E/eIF4G PPI-IN-1 (Compound A37) (25 mg/kg, 50 mg/kg, i.p., once a day, 18 days) inhibits the growth of HepG2 cells in HepG2 xenograft tumor mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 25 mg/kg, 50 mg/kg
Administration: i.p., once a day,18 days
Result: Reduced tumor growth, did not change weight and the shape of organ tissues.
Molecular Weight

430.31

Formula

C20H13Cl2N3O2S
SMILES

OC1=CC=C(C=C1)C2=CC=C(O2)/C=N/NC3=NC(C4=CC(Cl)=C(C=C4)Cl)=CS3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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eIF4E/eIF4G PPI-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

eIF4E/eIF4G PPI-IN-1Eukaryotic Initiation Factor (eIF)Bcl-2 FamilyApoptosisRasPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseInhibitorHela cellHepG2 cellMCF-7 cellHEK-293T cellHepG2 xenograft tumor mice modelinhibitorinhibit

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