| Size | Price | Stock | Qty |
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| Targets |
Morusin targets NF-κB and STAT3 as an inhibitor. It inhibits the phosphorylation of IKK-α, IKK-β, and IκB-β, increases expression of IκB-α, and suppresses nuclear translocation of NF-κB and its DNA binding activity. The compound activates caspases and restores GABA levels. It has anti-tumor, antioxidant, antibacterial, antinociceptive, analgesic, and anticonvulsant activities.
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| ln Vitro |
Morusin inhibits the growth of human and animal breast cancer cells in a dose- and time-dependent manner. The IC50 values for mouse breast cancer cells (4 T1 and EMT6), human breast cancer cells (MCF-7 and MDA-MB -231), and normal mammary epithelial cells (MCF-10A) are 2.03 and 1.87 μg/mL, respectively, and the maximum inhibition of cell growth (>80%) was found at 8 μg/mL. In a dose-dependent manner, apoptotic cells were markedly upregulated in breast cancer cells treated with morusin [1]. The proliferation and colony formation of human colorectal cancer HT-29 cells are markedly inhibited by muscin. Additionally, morusin promotes the production of IκB-α, suppresses the nuclear translocation of NF-κB and its DNA-binding activity, and inhibits the phosphorylation of IKK-α, IKK-β, and IκB-β. It was also demonstrated that the NF-κB upstream regulators Akt, PDK1, and PI3K were dephosphorylated. Moreover, early time points showed the activation of caspase-8, modifications to the mitochondrial membrane potential, the release of cytochrome c and Smac/DIABLO, and the activation of caspase-9 and -3. Following this, the expression of XIAP and Ku70 is downregulated [2]. Prostate cancer cells' ability to proliferate is inhibited by mususin, whereas normal human prostate epithelial cells are not significantly affected. By preventing STAT3 phosphorylation, nuclear accumulation, and DNA binding activity, morusin also lowers STAT3 activity. Moreover, the expression of STAT3 target genes that encode Cyclin D1, Bcl-xL, Bcl-2, Survivin, and c-Myc is downregulated by morusin. It lowers STAT3 activity, which causes human prostate cancer cells to undergo apoptosis [3].
In vitro, Morusin significantly inhibits the growth and clonogenicity of human colorectal cancer HT-29 cells. It inhibits the phosphorylation of IKK-α, IKK-β, and IκB-β, increases IκB-α expression, and suppresses NF-κB nuclear translocation and DNA binding activity. The compound shows anti-tumor effects on HT-29, A549, MCF-7, and MDA-MB-231 cell lines. It activates caspases and restores GABA levels. |
| ln Vivo |
Morusin dramatically reduces the rate at which breast cancer spreads. The tumor weights of mice administered 5 and 10 mg/kg morimulin were 0.61±0.23 and 0.41±0.10 g, respectively, and the tumor inhibition rates were 46.5% and 64.1%. The average tumor weight of control mice was 1.14±0.30 g. correspondingly [1].
In vivo, Morusin has anti-tumor activity in the treatment of prostate cancer. It significantly inhibits cell viability and reduces levels of inflammatory cytokines. The compound exhibits antinociceptive, analgesic, anticonvulsant, and antitumor activities. It is a prenylated flavonoid with diverse biological activities. Further in vivo studies are needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
In vitro enzyme assays for Morusin involve measuring NF-κB and STAT3 inhibition. NF-κB activity is assessed by measuring DNA binding activity or luciferase reporter gene assays. STAT3 phosphorylation is measured by Western blot. IKK-α, IKK-β, and IκB-β phosphorylation is assessed by Western blot. Caspase activity is measured using fluorogenic substrates. For antibacterial studies, MIC assays are performed. Assays are performed in appropriate buffer systems with positive controls.
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| Cell Assay |
In vitro cell-based assays for Morusin are conducted in cancer cell lines including HT-29, A549, MCF-7, and MDA-MB-231. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. NF-κB and STAT3 pathway activation is assessed by Western blot. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Morusin in vivo studies are conducted in animal models of cancer and inflammation. Tumor-bearing mice are treated with Morusin via oral administration or injection. Tumor growth is monitored by caliper measurements. For anti-inflammatory studies, inflammatory cytokine levels are measured. For antinociceptive and analgesic studies, pain models are used. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biomarker analysis at study endpoints.
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| ADME/Pharmacokinetics |
Morusin (MW 420.45 g/mol, C25H24O6) is a prenylated flavonoid. It is also known as Mulberrochromene. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. Morusin is used in anti-tumor, anti-inflammatory, and antibacterial research.
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| Toxicity/Toxicokinetics |
Morusin is generally well-tolerated in preclinical studies. The compound is a natural prenylated flavonoid from Morus alba with established safety profiles. Its anti-tumor, anti-inflammatory, and antibacterial activities have been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
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| Additional Infomation |
Phellinus linteus is an extended flavonoid with the following structure: hydroxyl groups are substituted at the 5', 2', and 4' positions, isopentenyl group at the 3' position, and 2,2-dimethylpyranyl group at the 7 and 8' positions. It is a plant metabolite and an antitumor drug. Phellinus linteus is a trihydroxyflavonoid and also an extended flavonoid. It has been reported to exist in mulberry (Morus lhou), Tokyo jackfruit (Artocarpus tonkinensis), and other organisms with relevant data.
Morusin (Mulberrochromene) is a prenylated flavonoid from Morus alba that inhibits NF-κB and STAT3. It inhibits IKK phosphorylation, suppresses NF-κB nuclear translocation, and activates caspases. The compound has anti-tumor (HT-29, A549, MCF-7, MDA-MB-231), antioxidant, antibacterial, antinociceptive, analgesic, and anticonvulsant activities. Its molecular formula is C25H24O6 with a molecular weight of 420.45 g/mol. All applications are limited to non-human research use. |
| Molecular Formula |
C25H24O6
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| Molecular Weight |
420.4545
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| Exact Mass |
420.157
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| CAS # |
62596-29-6
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| PubChem CID |
5281671
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
656.7±55.0 °C at 760 mmHg
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| Melting Point |
232-235ºC
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| Flash Point |
226.9±25.0 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
6.25
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
805
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XFFOMNJIDRDDLQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24O6/c1-13(2)5-7-17-22(29)21-19(28)12-20-16(9-10-25(3,4)31-20)24(21)30-23(17)15-8-6-14(26)11-18(15)27/h5-6,8-12,26-28H,7H2,1-4H3
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| Chemical Name |
2-(2,4-dihydroxyphenyl)-5-hydroxy-8,8-dimethyl-3-(3-methylbut-2-enyl)pyrano[2,3-h]chromen-4-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 : ≥ 100 mg/mL (~237.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 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 (5.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3784 mL | 11.8920 mL | 23.7840 mL | |
| 5 mM | 0.4757 mL | 2.3784 mL | 4.7568 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3784 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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