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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
MNK-8 targets the STAT3 protein, a transcription factor that is constitutively activated in many cancers and promotes cell proliferation, survival, and angiogenesis. MNK-8 inhibits STAT3 activation and its subsequent binding to DNA, thereby suppressing the transcription of downstream target genes involved in tumor progression.
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| ln Vitro |
In a time-dependent way, MNK8 (50 μM, 0-48 hours) boosts Sub-G1 cells and decreases the expression of anti-apoptotic proteins, including Bcl-2, survivin, and cyclin D1 [1].
In vitro, MNK-8 demonstrates good growth inhibitory activity against hepatocellular carcinoma (HCC) cells. At a concentration of 50 μM over a period of 0 to 48 hours, it results in a time-dependent increase in Sub-G1 cells, indicating apoptosis. Concurrently, it leads to a reduction in the levels of anti-apoptotic proteins, namely Bcl-2, survivin, and cyclin D1. MNK8 reduces prosurvivin expression and migration/invasion of HCC cells. |
| ln Vivo |
In vivo activity data for MNK-8 are limited in the available literature. However, based on its potent in vitro activity against HCC cells, it is anticipated to have potential in vivo antitumor efficacy.
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| Enzyme Assay |
Non-cellular assays for MNK-8 typically involve measuring its inhibition of STAT3 binding to DNA. This is often performed using an electrophoretic mobility shift assay (EMSA) or a DNA-binding ELISA, where the compound's ability to prevent STAT3 from binding to its consensus DNA sequence is assessed.
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| Cell Assay |
In vitro cellular assays for MNK-8 commonly use hepatocellular carcinoma (HCC) cell lines. Cells are treated with various concentrations of MNK-8, and cell viability is assessed using assays like MTT. Apoptosis is evaluated by flow cytometry to measure Sub-G1 cell populations. The expression of STAT3 target genes, such as Bcl-2, survivin, and cyclin D1, is analyzed by Western blotting.
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| Animal Protocol |
In vivo animal studies for MNK-8 are not extensively documented. Based on its activity against HCC cells, typical study designs would involve xenograft mouse models. Tumor-bearing mice would be administered MNK-8, and tumor growth inhibition would be monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MNK-8 are not extensively characterized. As a small molecule with a molecular weight of 252.27 and a LogP of 2.1, it is soluble in DMSO (~41.67 mg/mL).
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| Toxicity/Toxicokinetics |
Specific toxicological data for MNK-8 are limited. As a research compound, comprehensive toxicity profiles are not available. It is intended for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
MNK-8 is a research-grade compound for laboratory use only and is not approved for clinical use. Its primary application is in cancer research, specifically for studying the STAT3 signaling pathway in hepatocellular carcinoma and other cancers. It is a valuable tool for investigating the therapeutic potential of STAT3 inhibitors.
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| Molecular Formula |
C15H12N2O2
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|---|---|
| Molecular Weight |
252.27
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| Exact Mass |
252.09
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| Elemental Analysis |
C, 71.42; H, 4.79; N, 11.10; O, 12.68
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| CAS # |
2055078-49-2
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| PubChem CID |
164517038
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
430
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C(=O)C=C(NC1=O)C2=CC=CC3=CC=CC=C32
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| InChi Key |
SJRMGNRXVMMJSY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12N2O2/c1-17-14(18)9-13(16-15(17)19)12-8-4-6-10-5-2-3-7-11(10)12/h2-9H,1H3,(H,16,19)
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| Chemical Name |
3-methyl-6-naphthalen-1-yl-1H-pyrimidine-2,4-dione
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| Synonyms |
MNK8; MNK 8; MNK-8;
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~41.67 mg/mL (~165.18 mM)
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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 | 3.9640 mL | 19.8200 mL | 39.6401 mL | |
| 5 mM | 0.7928 mL | 3.9640 mL | 7.9280 mL | |
| 10 mM | 0.3964 mL | 1.9820 mL | 3.9640 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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