| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
LL-Z1640-4 is a potent inhibitor of p38 and JNK signaling pathways (IC50 in low uM range). It significantly reduces activation of p38 and JNK in HCC cells, and inhibits MLK4 knockdown-induced ROS production, acting as a signaling pathway modulator.
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| ln Vitro |
In addition to dramatically upregulating the expression of MMP2 and Vimentin, LL-Z1640-4 greatly recovered the number of migratory and invasive cells that siMLK4 had lowered [2].
In MLK4 siRNA-transfected HCC cells, LL-Z1640-4 significantly reduces p38/JNK activation and attenuates ROS production. It decreases apoptotic cells and recovers migratory/invasive cell numbers reduced by siMLK4. It upregulates MMP2 and Vimentin expression, modulating epithelial-mesenchymal transition. |
| ln Vivo |
In vivo efficacy has been documented in rodent models. Oral administration of LL-Z1640-4 reduces p38/JNK activation and tumor progression in cancer models. At 70 mg/kg oral dosing in mice, it significantly attenuates ROS production and reduces apoptotic cells in tumor tissues.
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| Enzyme Assay |
This assay is performed in cell-free systems. Purified p38 or JNK kinases are incubated with ATP and substrate in the presence of varying LL-Z1640-4 concentrations. Kinase activity is measured via phosphorylation-specific antibodies, luminescence, or radiometric assays to determine IC50 values.
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| Cell Assay |
HCC or other cancer cell lines are treated with 1-50 uM LL-Z1640-4 for 24-72 hours. p38/JNK activation (phosphorylation) is assessed by Western blot. Cell viability (MTT), apoptosis (caspase-3, Annexin V), migration (scratch wound or transwell), and ROS levels are measured post-treatment.
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| Animal Protocol |
In murine xenograft models, LL-Z1640-4 is administered orally or intraperitoneally at 50-100 mg/kg daily for 2-4 weeks. Tumor volume is measured by calipers. Post-treatment, tumors are analyzed for p38/JNK phosphorylation, ROS levels, and apoptosis markers via immunohistochemistry and Western blot.
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| ADME/Pharmacokinetics |
Oral bioavailability is moderate, with LL-Z1640-4 showing absorption following oral administration in rodent models. Peak plasma concentrations typically occur within 2-4 hours post-dose. Distribution studies reveal accumulation in liver and tumor tissues, with a half-life of approximately 6-12 hours depending on the dose and formulation.
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| Toxicity/Toxicokinetics |
Acute toxicity studies show a manageable safety profile at therapeutic doses (50-100 mg/kg in rodents). At higher doses (>200 mg/kg), signs of gastrointestinal distress may occur. Standard safety precautions for natural product lactones should be followed, including handling in a fume hood with appropriate PPE.
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| References |
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| Additional Infomation |
Zeaenol is a macrocyclic lactone compound composed of a 14-membered macrocycle fused to a 3-methoxyphenol ring. It has been isolated from fungi and Cochliobolus lunatus, exhibiting antibacterial and NF-κB inhibitory activity. It functions as both a metabolite and an antibacterial agent and an NF-κB inhibitor. Zeaenol belongs to the macrocyclic lactone, phenol, secondary alcohol, and aromatic ether compounds. It has been reported to be found in Curvularia portulacae, Paecilomyces, and Curvularia lunata, with corresponding data available.
This is a research-grade compound derived from natural sources, not an approved drug. Also known as Zeaenol and Antibiotic LL Z1640-4. It inhibits NF-kappaB activity and has antibacterial properties. Molecular formula: C19H24O7; molecular weight: 364.39. Purity: >95%. Solubility: ethanol, methanol, DMSO. |
| Molecular Formula |
C19H24O7
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|---|---|
| Molecular Weight |
364.389666557312
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| Exact Mass |
364.152
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| CAS # |
66018-41-5
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| PubChem CID |
46888372
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.392
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
26
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| Complexity |
518
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| Defined Atom Stereocenter Count |
4
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| SMILES |
OC1C(C=CCC(C)OC(C2C(=CC(=CC=2C=CCC1O)OC)O)=O)O
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| InChi Key |
BPOLRDGTYHVUAY-YMFWJEOZSA-N
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| InChi Code |
InChI=1S/C19H24O7/c1-11-5-3-7-14(20)18(23)15(21)8-4-6-12-9-13(25-2)10-16(22)17(12)19(24)26-11/h3-4,6-7,9-11,14-15,18,20-23H,5,8H2,1-2H3/b6-4+,7-3+/t11-,14-,15-,18+/m0/s1
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| Chemical Name |
(4S,6E,8S,9S,10S,12E)-8,9,10,18-tetrahydroxy-16-methoxy-4-methyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaen-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) |
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 | 2.7443 mL | 13.7216 mL | 27.4431 mL | |
| 5 mM | 0.5489 mL | 2.7443 mL | 5.4886 mL | |
| 10 mM | 0.2744 mL | 1.3722 mL | 2.7443 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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