1. MAPK/ERK Pathway Cell Cycle/DNA Damage Apoptosis
  2. MNK Eukaryotic Initiation Factor (eIF) Apoptosis
  3. EB1

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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EB1 Chemical Structure

EB1 Chemical Structure

CAS No. : 42951-68-8

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Description

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[1][2].

IC50 & Target[1]

MNK1

0.69 μM (IC50)

MNK2

9.4 μM (IC50)

eIF4E

 

Cellular Effect
Cell Line Type Value Description References
IMR-90 GI50
> 40 μM
Compound: 6b; EB1
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
[PMID: 35417652]
MCF7 GI50
8.46 μM
Compound: 6b; EB1
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
[PMID: 35417652]
MDA-MB-231 GI50
15.08 μM
Compound: 6b; EB1
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
[PMID: 35417652]
MDA-MB-468 GI50
14.46 μM
Compound: 6b; EB1
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
[PMID: 35417652]
In Vitro

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.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells
Concentration: 1.3 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 24 hours
Result: Blocked the phosphorylation of eIF4E in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells
Concentration: 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 72 hours
Result: Increased the percentage of apoptosis cells among tumor cells.
Molecular Weight

286.33

Formula

C18H14N4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=NNC2=C1C(C3=CC=CC=C3)=CC(C4=CC=CC=C4)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4925 mL 17.4624 mL 34.9247 mL
5 mM 0.6985 mL 3.4925 mL 6.9849 mL
View the 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.

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Purity & Documentation
References

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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  • 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.

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EB1
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