| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
The primary target of Kansuinin A is the IL-6/STAT3 signaling pathway. IL-6 is a pro-inflammatory cytokine that activates STAT3 (signal transducer and activator of transcription 3), a transcription factor involved in cell proliferation, survival, and inflammation. Kansuinin A inhibits IL-6-induced STAT3 activation by activating ERK1/2. By inhibiting STAT3 activation, the compound suppresses pro-inflammatory cytokine production and exerts antiviral and anticancer effects. It has also been shown to modulate gut microbiota and related metabolic functions.
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|---|---|
| ln Vitro |
In vitro, Kansuinin A inhibits IL-6-induced STAT3 activation. It has antiviral and anticancer activity. The compound reduces oxidative stress and suppresses pro-inflammatory cytokine production. As a diterpenoid, it may have additional activities related to its structural properties. However, specific IC₅₀ values or detailed activity data is not provided in the available sources.
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| ln Vivo |
In vivo, Kansuinin A has been shown to ameliorate malignant ascites by modulating gut microbiota and related metabolic functions. It has also shown promise in reducing oxidative stress, suppressing pro-inflammatory cytokine production, and protecting neurons from damage. Its ability to inhibit IL-6/STAT3 signaling suggests potential therapeutic applications in inflammatory diseases, cancer, and neurodegenerative disorders. However, specific in vivo dosing and efficacy data is not detailed in the available sources.
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| Enzyme Assay |
For STAT3 inhibitors, standard cell-free assays involve measuring STAT3 DNA binding activity using electrophoretic mobility shift assays (EMSA) or ELISA-based assays. The compound is incubated with STAT3 protein and a STAT3-binding oligonucleotide, and DNA binding is measured.
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| Cell Assay |
For STAT3 inhibitors, standard cellular assays involve treatment of cancer cell lines with the test compound for 24-72 hours. STAT3 phosphorylation (Tyr705) is measured by western blot. STAT3 target gene expression (e.g., Bcl-2, Mcl-1, Cyclin D1) is measured by qPCR. Cell viability (MTT or CellTiter-Glo), apoptosis, and proliferation are assessed.
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| Animal Protocol |
For in vivo evaluation of STAT3 inhibitors, standard animal models include tumor xenograft models, models of inflammation, and neurodegenerative disease models. The compound is typically administered orally or intraperitoneally, and tumor growth, inflammation markers, STAT3 phosphorylation, and survival are assessed.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Kansuinin A is not provided in the available sources. The compound has a molecular formula of C₃₉H₄₆O₁₅. As a diterpenoid with moderate lipophilicity, it would be expected to have reasonable oral absorption. Comprehensive PK studies would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for Kansuinin A is not provided in the available sources. As a naturally occurring compound, it may have a favorable safety profile at moderate doses. However, comprehensive toxicological evaluation would be required for therapeutic development. The compound is for research use only and not for therapeutic applications.
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| References | |
| Additional Infomation |
Reports indicate that plants in the Euphorbia genus contain euphorbia glycoside A, and relevant data is available for reference.
Kansuinin A is a diterpenoid compound isolated from Euphorbia kansui that primarily targets the IL-6 pathway. It inhibits IL-6-induced STAT3 activation and possesses antiviral and anticancer activity. The compound has been shown to ameliorate malignant ascites by modulating gut microbiota. No regulatory approval has been identified. |
| Molecular Formula |
C37H46O15
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|---|---|
| Molecular Weight |
730.76
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| Exact Mass |
730.284
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| CAS # |
57701-86-7
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| PubChem CID |
11366139
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| Appearance |
White to off-white solid powder
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| LogP |
2.785
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
52
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| Complexity |
1480
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@H]1C[C@]2([C@H]([C@H]1OC(=O)C)[C@H](C(=C)[C@@H]([C@H]([C@H](C([C@@H]3C(=O)[C@H]([C@]2(O3)O)C)(C)C)OC(=O)C)OC(=O)C4=CC=CC=C4)OC(=O)C)OC(=O)C)OC(=O)C
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| InChi Key |
VKHCUWUNVKZFBM-PNKWBUBPSA-N
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| InChi Code |
InChI=1S/C37H46O15/c1-17-16-36(51-24(8)42)26(28(17)46-20(4)38)29(47-21(5)39)18(2)30(48-22(6)40)31(50-34(44)25-14-12-11-13-15-25)33(49-23(7)41)35(9,10)32-27(43)19(3)37(36,45)52-32/h11-15,17,19,26,28-33,45H,2,16H2,1,3-10H3/t17-,19+,26+,28-,29-,30-,31+,32-,33+,36+,37+/m0/s1
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| Chemical Name |
[(1R,2R,4S,5S,6R,7R,9S,10S,11S,13R,15R)-2,5,7,9,11-pentaacetyloxy-1-hydroxy-4,12,12,15-tetramethyl-8-methylidene-14-oxo-16-oxatricyclo[11.2.1.02,6]hexadecan-10-yl] benzoate
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| Synonyms |
Kansuinin A; Kansuinine A
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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 : ≥ 100 mg/mL (~136.85 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3684 mL | 6.8422 mL | 13.6844 mL | |
| 5 mM | 0.2737 mL | 1.3684 mL | 2.7369 mL | |
| 10 mM | 0.1368 mL | 0.6842 mL | 1.3684 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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