| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 25mg | |||
| Other Sizes |
| Targets |
STAT3 (signal transducer and activator of transcription 3); MEG2 (protein tyrosine phosphatase).
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|---|---|
| ln Vitro |
Methyllucidone is a STAT3 inhibitor that acts by regulating the expression of the protein tyrosine phosphatase MEG2. It strongly inhibits the growth of human cancer cells. The antitumor effects are further confirmed with caspase-3 activation and degradation of PARP. Methyllucidone may have neuroprotective potential via inhibition of neurotoxic microglial activation.
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| ln Vivo |
Methyllucidone strongly inhibits the growth of human cancer cells and colon tumor xenografts in nude mice. The antitumor effects are confirmed with caspase-3 activation and degradation of PARP. The compound may have neuroprotective potential in vivo via inhibition of neurotoxic microglial activation. Further in vivo studies would be needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays measure STAT3 inhibition and MEG2 regulation. Recombinant STAT3 protein or cell lysates are incubated with Methyllucidone at varying concentrations (typically 0.1-100 µM). STAT3 phosphorylation and DNA-binding activity are assessed by Western blot and EMSA. MEG2 phosphatase activity is measured using a phosphatase assay with appropriate substrates. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays are performed using cancer cell lines (e.g., colon cancer, breast cancer) or microglial cell lines. Cells are treated with Methyllucidone at concentrations ranging from 0.1-100 µM for 24-72 hours. STAT3 phosphorylation and target gene expression are measured by Western blot and qRT-PCR. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is measured by Annexin V/PI staining, caspase-3/7 activity, and PARP cleavage. Neuroprotection is assessed in microglial activation models.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models using human colon cancer cells. Methyllucidone is administered orally or intraperitoneally at doses ranging from 1-50 mg/kg. Tumor volume is measured by caliper twice weekly. STAT3 phosphorylation and downstream markers are assessed in tumor tissues by immunohistochemistry and Western blot. Apoptosis is confirmed by TUNEL staining and caspase-3 activation. Body weight and clinical signs are monitored.
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| ADME/Pharmacokinetics |
Methyllucidone has a molecular weight of 270.28 g/mol and molecular formula C16H14O4. CAS number: 19956-54-8. Purity ≥98%. Store as a powder at -20°C. Soluble in DMSO. For in vivo use, formulate in suitable vehicle. The compound is stable for up to 2 years when stored desiccated at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for Methyllucidone. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments would include cytotoxicity profiling, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential. The compound is for research use only.
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| References | |
| Additional Infomation |
Methylluxone belongs to the chalcone class of compounds and has antioxidant properties. (Structure can be found in the first source.)
Methyllucidone is a research-grade STAT3 inhibitor with antitumor and potential neuroprotective activities. It is not approved for clinical use. The compound is also known as methyl lucidone. It inhibits STAT3 by regulating MEG2 expression. Methyllucidone strongly inhibits the growth of human cancer cells and colon tumor xenografts. It is supplied as a powder with high purity and should be stored desiccated at -20°C. Bioorg Med Chem Lett, 2018, 28(5):853-857. |
| Molecular Formula |
C22H34N4O5S2CL2
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|---|---|
| Molecular Weight |
569.56516
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| Exact Mass |
270.089
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| CAS # |
19956-54-8
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| PubChem CID |
21680425
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
514.0±50.0 °C at 760 mmHg
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| Flash Point |
231.0±30.2 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.581
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| LogP |
2.19
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
491
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=O)/C(=C(\C=C\C2=CC=CC=C2)/OC)/C1=O
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| InChi Key |
FITVJPYUOAZKPN-PBMBQWDMSA-N
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| InChi Code |
InChI=1S/C16H14O4/c1-19-13(9-8-11-6-4-3-5-7-11)15-12(17)10-14(20-2)16(15)18/h3-10H,1-2H3/b9-8+,15-13-
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| Chemical Name |
(2Z)-4-methoxy-2-[(E)-1-methoxy-3-phenylprop-2-enylidene]cyclopent-4-ene-1,3-dione
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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) |
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 | 1.7557 mL | 8.7786 mL | 17.5571 mL | |
| 5 mM | 0.3511 mL | 1.7557 mL | 3.5114 mL | |
| 10 mM | 0.1756 mL | 0.8779 mL | 1.7557 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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