EB1
Based on 1 Customer Validation
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.
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- Pureza: 99.91%
- No. CAS: 42951-68-8
- Fòrmula: C18H14N4
- Peso molecular:286.33
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
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Actividad biológica
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MNK1 0.69 μM (IC50) |
MNK2 9.4 μM (IC50) |
eIF4E |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-90 | GI50 |
>40 μM
Compound: 6b; EB1
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Cytotoxicity against human IMR-90 cells assessed as reduction in cell viability measured after 72 hrs by crystal violet staining based assay
Cytotoxicity against human IMR-90 cells assessed as reduction in cell viability measured after 72 hrs by crystal violet staining based assay
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[PMID: 35417652] |
| MCF7 | GI50 |
8.46 μM
Compound: 6b; EB1
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Growth inhibition of human MCF7 cells measured after 72 hrs by crystal violet staining based assay
Growth inhibition of human MCF7 cells measured after 72 hrs by crystal violet staining based assay
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[PMID: 35417652] |
| MDA-MB-231 | GI50 |
15.08 μM
Compound: 6b; EB1
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Growth inhibition of human MDA-MB-231 cells measured after 72 hrs by crystal violet staining based assay
Growth inhibition of human MDA-MB-231 cells measured after 72 hrs by crystal violet staining based assay
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[PMID: 35417652] |
| MDA-MB-468 | GI50 |
14.46 μM
Compound: 6b; EB1
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Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by crystal violet staining based assay
Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by crystal violet staining based assay
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[PMID: 35417652] |
EB1 (1.3-40 μM; 24 hr) inhibits the phosphorylation of eIF4E dose-dependently[1].
EB1 (2.5-40 μM; 72 hr) shows dose-dependent cytotoxicity on tumor cells, and induces apoptosis[1].
EB1 (5 μM, 10 μM, and 20 μM; 24 hr) acts directly on MNK kinases without perturbing activating upstream signaling, such as activation of p38 (p-p38) and phosphorylation of its downstream effector HSP27[1].
EB1 (compound 14) inhibits the growth of HepG2 and MCF-7 cancer cells with IC50s of 0.74 μM and 5.18 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells
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Concentration:1.3 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
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Incubation Time:24 hours
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Result:Blocked the phosphorylation of eIF4E in a dose-dependent manner.
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Cell Line:MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells
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Concentration:2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
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Incubation Time:72 hours
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Result:Increased the percentage of apoptosis cells among tumor cells.
Chemical Information
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No. CAS 42951-68-8
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Appearance Solid
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Peso molecular 286.33
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Fòrmula C18H14N4
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Color Light yellow to yellow
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SMILES
NC1=NNC2=C1C(C3=CC=CC=C3)=CC(C4=CC=CC=C4)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 8.33 mg/mL (29.09 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bou-Petit E, et al. Overcoming Paradoxical Kinase Priming by a Novel MNK1 Inhibitor. J Med Chem. 2022 Apr 28;65(8):6070-6087. [Content Brief]
[2]. Aboukhatwa SM, et al. Nicotinonitrile-derived apoptotic inducers: Design, synthesis, X-ray crystal structure and Pim kinase inhibition. Bioorg Chem. 2022 Dec;129:106126. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL | 87.3118 mL |
| 5 mM | 0.6985 mL | 3.4925 mL | 6.9849 mL | 17.4624 mL | |
| 10 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL | 8.7312 mL | |
| 15 mM | 0.2328 mL | 1.1642 mL | 2.3283 mL | 5.8208 mL | |
| 20 mM | 0.1746 mL | 0.8731 mL | 1.7462 mL | 4.3656 mL | |
| 25 mM | 0.1397 mL | 0.6985 mL | 1.3970 mL | 3.4925 mL |
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