| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
MNK1 0.69 μM (IC50) MNK2 9.4 μM (IC50) eIF4E
EB1 targets MNK1 and MNK2 kinases, which are downstream effectors of the MAPK/ERK signaling pathway. MNK kinases phosphorylate eukaryotic initiation factor 4E (eIF4E) at Ser209, which promotes cap-dependent mRNA translation and is involved in cancer cell proliferation and survival. By inhibiting MNK1 and MNK2, EB1 suppresses eIF4E phosphorylation, leading to reduced translation of oncogenic mRNAs and induction of apoptosis. The compound selectively inhibits the growth of cancer cells but not normal cells. |
|---|---|
| ln Vitro |
EB1 (1.3–40 μM; 24 hours) suppresses eIF4E phosphorylation in a dose-dependent manner [1]. EB1 (2.5–40 μM; 72 hours) causes tumor cells to undergo apoptosis and exhibits dose-dependent cytotoxicity [1]. After acting on MNK kinase for 24 hours at concentrations of 5 μM, 10 μM, and 20 μM, EB1 does not interfere with the activation of upstream signals, such as p38 (p-p38) activation or the phosphorylation of its downstream effector HSP27 [1]. Compound 14 (EB1) has an inhibitory concentration of 0.74 μM and 5.18 μM on HepG2 and MCF-7 cancer cells, respectively[2].
In vitro studies demonstrate that EB1 inhibits MNK1 and MNK2 with IC50 values of 0.69 μM and 9.4 μM, respectively. EB1 selectively inhibits the growth of cancer cells but not normal cells. The compound increases cell apoptosis and suppresses eIF4E phosphorylation. The compound's selectivity for cancer cells over normal cells makes it a valuable tool for studying MNK signaling in cancer biology. |
| ln Vivo |
No detailed in vivo activity data has been published for EB1. The compound has been primarily characterized in vitro as a research tool for studying MNK kinase signaling and cancer biology. Its ability to selectively inhibit cancer cell growth and induce apoptosis suggests that it could have potential for in vivo applications. Further studies would be needed to evaluate its efficacy in animal models of cancer.
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| Enzyme Assay |
The MNK inhibitory activity of EB1 can be assessed using in vitro kinase assays. In a typical assay, recombinant MNK1 or MNK2 kinase is incubated with a peptide substrate (such as eIF4E peptide), ATP (including radiolabeled ³³P-ATP), and varying concentrations of EB1. The incorporation of phosphate into the substrate is measured, and the IC50 is calculated. The IC50 for MNK1 is 0.69 μM and for MNK2 is 9.4 μM. The selectivity against other kinases can be assessed using kinase profiling services.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells Tested Concentrations: 1.3 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Blocked the phosphorylation of eIF4E in a dose-dependent manner. Apoptosis Analysis[1] Cell Types: MDA-MB-231, MDA -MB-468, MCF7, and IMR90 cells Tested Concentrations: 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM Incubation Duration: 72 hrs (hours) Experimental Results: Increased the percentage of apoptosis cells among tumor cells. The cellular activity of EB1 is assessed using cancer cell lines and normal cells. Cells are treated with varying concentrations of EB1. eIF4E phosphorylation is assessed by Western blotting using phospho-specific antibodies for eIF4E (Ser209). Apoptosis is assessed by annexin V/propidium iodide staining or caspase activation assays. Cell viability is measured using MTT or CellTiter-Glo assays. The selectivity of EB1 for cancer cells over normal cells is confirmed by comparing activity against cancer cell lines and normal cell lines. |
| Animal Protocol |
No detailed in vivo animal model data has been published for EB1. The compound has been primarily characterized in vitro as a research tool for studying MNK signaling. Future studies may involve the use of mouse xenograft models of cancer to assess the in vivo efficacy of EB1. The compound's selectivity for cancer cells over normal cells suggests that it may have a favorable safety profile.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for EB1. The compound has a molecular weight of 286.33 and a molecular formula of C18H14N4. It has a purity of ≥99%. The compound is soluble in DMSO. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties, including oral bioavailability, plasma protein binding, clearance, and half-life.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for EB1. The compound selectively inhibits the growth of cancer cells but not normal cells, suggesting a favorable selectivity profile. As an MNK inhibitor, the compound may have on-target effects on eIF4E-mediated translation in normal tissues. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
EB1 (CAS# 42951-68-8) is a potent and selective MNK kinase inhibitor with IC50 values of 0.69 μM for MNK1 and 9.4 μM for MNK2. The compound selectively inhibits the growth of cancer cells but not normal cells, increases cell apoptosis, and suppresses eIF4E phosphorylation. The molecular formula is C18H14N4 and molecular weight is 286.33. EB1 is a research tool for studying MNK signaling and cancer biology.
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| Molecular Formula |
C18H14N4
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|---|---|
| Molecular Weight |
286.33
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| Exact Mass |
286.122
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| Elemental Analysis |
C, 75.50; H, 4.93; N, 19.57
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| CAS # |
42951-68-8
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| PubChem CID |
2048804
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.455
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
362
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C2=CC(C3=CC=CC=C3)=NC3=NNC(N)=C23)=CC=CC=C1
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| InChi Key |
NGNHXYCLUMQSKR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14N4/c19-17-16-14(12-7-3-1-4-8-12)11-15(20-18(16)22-21-17)13-9-5-2-6-10-13/h1-11H,(H3,19,20,21,22)
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| Chemical Name |
4,6-Diphenyl-2H-pyrazolo[3,4-b]pyridin-3-amine
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| Synonyms |
E-B1, E-B-1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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