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| Targets |
Nigakinone targets multiple biological targets including Cyclin G-associated Kinase (GAK) and Schistosoma Mansoni Peroxiredoxins. It exhibits inhibitory effects on a diverse range of biological targets. As an NSAID-like compound, it may also target cyclooxygenase pathways. Its anti-inflammatory, antimicrobial, and anticancer activities are mediated through these targets. The compound is a natural product with diverse bioactivities.
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| ln Vitro |
In vitro, Nigakinone shows cytotoxicity against human CNE-2 cells with an IC₅₀ value of 7.96 μg/mL. It has been shown to have anti-inflammatory and anticancer properties in cell culture models. The compound's effects on chronic arthritis, inflammatory bowel disease, and skin cancer have been evaluated in vitro. It exhibits antimicrobial activity against various pathogens. Detailed in vitro data are available in the natural products literature.
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| ln Vivo |
In vivo, Nigakinone has been evaluated for its anti-inflammatory and anticancer effects in animal models. It has shown potential for treating ulcerative colitis, chronic arthritis, inflammatory bowel disease, and skin cancer. The compound is a natural product with pharmacological activities. Further in vivo studies are needed to fully characterize its efficacy and safety.
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| Enzyme Assay |
In vitro assays for Nigakinone typically measure anti-inflammatory, antimicrobial, and anticancer activities. Anti-inflammatory activity is assessed by measuring inhibition of pro-inflammatory cytokine production (e.g., TNF-α, IL-6) in LPS-stimulated macrophages. Antimicrobial activity is assessed by broth microdilution methods against bacterial or fungal strains. Anticancer activity is assessed by MTT or CellTiter-Glo assays in cancer cell lines (e.g., CNE-2). IC₅₀ values are calculated from dose-response curves. Controls include vehicle and reference compounds.
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| Cell Assay |
For cell-based assays, relevant cell lines (e.g., CNE-2 cancer cells, macrophages, or inflammatory bowel disease models) are cultured in DMEM or RPMI-1640 with 10% FBS. Cells are seeded in 96-well plates and treated with Nigakinone at various concentrations for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo. Cytokine levels are measured by ELISA. Apoptosis is assessed by flow cytometry or caspase assays. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, Nigakinone may be administered orally or intraperitoneally to rodents. For ulcerative colitis models, compound is administered during disease induction. Disease activity index, colon length, and histological scores are assessed. Inflammatory cytokine levels in colon tissue are measured by ELISA. For cancer models, tumor volume and survival are monitored. All procedures follow institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Nigakinone (MW 266.25, C₁₅H₁₀N₂O₃) is a natural alkaloid. The compound is isolated from plant sources. Its physicochemical properties have been characterized. Pharmacokinetic properties in animals have been studied. The compound is for research use only. Further studies are needed to fully characterize its ADME profile.
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| Toxicity/Toxicokinetics |
Nigakinone has been evaluated for toxicity in preclinical studies. As a natural product with NSAID-like activity, gastrointestinal effects may occur. The compound has shown cytotoxicity against cancer cells. Standard safety pharmacology studies would be required for therapeutic development. The compound is for research use only and not intended for human therapeutic applications.
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| References |
: Quality
Assessment of Kumu Injection, a Traditional Chinese Medicine
Preparation, Using HPLC Combined with Chemometric Methods and
Qualitative and Quantitative Analysis of Multiple Alkaloids by Single
Marker. Molecules. 2018 Apr 9;23(4).; Gong G, Jiang L, Lin Q, Liu W, He MF, Zhang J, Feng F, Qu W, Xie N. In vivo toxic effects of 4-methoxy-5-hydroxy-canthin-6-one in zebrafish embryos via copper dyshomeostasis and oxidative stress. Comp Biochem Physiol C Toxicol Pharmacol. 2018 Jan;204:79-87. doi: 10.1016/j.cbpc.2017.11.014. Epub 2017 Dec 5. PubMed PMID: 29208543.
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| Additional Infomation |
Nigarone belongs to the β-carboline class of compounds. It has been reported that nigarone is found in Quassia amara, Picrasma excelsa, and Picrasma quassioides, and relevant data are available for reference.
Nigakinone is a research-grade natural alkaloid with anti-inflammatory, antimicrobial, and anticancer properties. Its primary applications include natural products research, pharmacology, and drug discovery. The compound is not approved for clinical use. It is commercially available from chemical suppliers for research purposes only. Its mechanism involves multiple biological targets. |
| Molecular Formula |
C15H10N2O3
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|---|---|
| Molecular Weight |
266.2515
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| Exact Mass |
266.069
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| CAS # |
18110-86-6
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| PubChem CID |
5320161
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
442.7±45.0 °C at 760 mmHg
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| Flash Point |
221.5±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.747
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| LogP |
1.92
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
476
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PGFKZUOYIFDMQJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10N2O3/c1-20-14-11-12-9(6-7-16-11)8-4-2-3-5-10(8)17(12)15(19)13(14)18/h2-7,18H,1H3
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| Chemical Name |
3-hydroxy-4-methoxy-1,6-diazatetracyclo[7.6.1.05,16.010,15]hexadeca-3,5(16),6,8,10,12,14-heptaen-2-one
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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) |
DMSO : ~8.33 mg/mL (~31.29 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 | 3.7559 mL | 18.7793 mL | 37.5587 mL | |
| 5 mM | 0.7512 mL | 3.7559 mL | 7.5117 mL | |
| 10 mM | 0.3756 mL | 1.8779 mL | 3.7559 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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