| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg | |||
| Other Sizes |
| Targets |
Destruxin A targets vacuolar-type H+-ATPase (V-ATPase), a multi-subunit enzyme that pumps protons across membranes to acidify intracellular compartments. V-ATPase is essential for various cellular processes, including endocytosis, protein degradation, and neurotransmitter release. By inhibiting V-ATPase, Destruxin A disrupts these processes, leading to cell death. The compound also exhibits immunosuppressive effects by inhibiting T cell proliferation and cytokine production. Its insecticidal activity is attributed to its effects on insect midgut cells and V-ATPase inhibition.
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| ln Vitro |
In vitro studies have demonstrated that Destruxin A is a potent inhibitor of V-ATPase, with IC50 values in the low micromolar range. The compound exhibits insecticidal activity against various insect pests and has been shown to inhibit the growth of cancer cell lines. Destruxin A also exhibits immunosuppressive effects by inhibiting T cell proliferation and cytokine production. The compound's antiviral activity has been demonstrated against various viruses. These in vitro activities support the compound's potential applications in agriculture, pharmacology, and cancer research.
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| ln Vivo |
In vivo studies have demonstrated that Destruxin A is effective as a biological insecticide against various agricultural pests. The compound has been shown to cause rapid paralysis and death in insects following ingestion or injection. Destruxin A has also been studied for its anticancer and immunosuppressive effects in animal models. However, detailed in vivo efficacy data, including dose-response relationships and specific animal model studies, are not widely available in the published literature. Further studies are needed to fully characterize the in vivo pharmacological profile of this compound.
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| Enzyme Assay |
The in vitro enzyme assay for Destruxin A typically involves measuring the inhibition of V-ATPase activity using purified V-ATPase enzyme preparations or membrane vesicles containing V-ATPase. The assay is performed in a buffer system optimized for V-ATPase activity, with the compound added at varying concentrations to determine the IC50 value. The reaction is initiated by the addition of ATP, and the amount of inorganic phosphate released is quantified using a colorimetric detection method. IC50 values are calculated by fitting the inhibition data to a sigmoidal dose-response curve.
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| Cell Assay |
Cellular assays for Destruxin A are conducted using various cell lines, including insect cells, cancer cells, and immune cells. Cells are treated with varying concentrations of the compound, and cell viability, proliferation, and apoptosis are assessed. For immunosuppressive studies, T cells are treated with Destruxin A, and proliferation and cytokine production are measured. For anticancer studies, cancer cell viability is assessed using MTT or other assays. These cell-based assays confirm the compound's biological activities and provide insights into its mechanism of action.
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| Animal Protocol |
In vivo animal studies for Destruxin A are conducted in insect models for insecticidal activity and in mouse models for anticancer and immunosuppressive studies. For insecticidal studies, insects are treated with Destruxin A orally or by injection, and mortality is monitored. For anticancer studies, mice bearing tumors are treated with Destruxin A, and tumor growth is monitored. For immunosuppressive studies, mice are treated with Destruxin A, and immune responses are assessed. These studies confirm the compound's in vivo efficacy and support its potential applications.
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| ADME/Pharmacokinetics |
Destruxin A has a molecular weight of approximately 579.73 and a molecular formula of C29H49N5O7. The compound is soluble in DMSO and other organic solvents. For research use, Destruxin A is typically stored as powder at -20degC for up to 3 years or at 4degC for up to 2 years, and in solvent at -80degC for up to 1 year. Detailed pharmacokinetic parameters such as oral bioavailability, half-life, and tissue distribution have not been determined for this compound.
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| Toxicity/Toxicokinetics |
Destruxin A is a mycotoxin with insecticidal and immunosuppressive properties. As a toxin, the compound can be toxic to cells and tissues at high concentrations. The compound has been studied for its potential as a biological insecticide, but its toxicity to non-target organisms, including mammals, is a concern. Standard safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
Destruxin A is a cyclic condensate. It has been reported to be found in Metarhizium indigoticum, Metarhizium anisopliae, and Trichothecium roseum, and relevant data are available for reference.
Destruxin A (CAS#: 6686-70-0) is a cyclic depsipeptide mycotoxin produced by Metarhizium anisopliae, a fungus used as a biological insecticide. It has a molecular formula of C29H49N5O7 and a molecular weight of approximately 579.73. The compound inhibits V-ATPase, disrupting intracellular acidification and cellular processes. Destruxin A exhibits insecticidal, immunosuppressive, antiviral, and anticancer activities. It is not approved for clinical use and is available only for research purposes in entomology, pharmacology, and cancer research. |
| Molecular Formula |
C29H47N5O7
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|---|---|
| Molecular Weight |
577.71278
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| Exact Mass |
577.348
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| CAS # |
6686-70-0
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| PubChem CID |
11421831
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| Appearance |
White to off-white solid powder
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| LogP |
1.211
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
41
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC[C@H](C)[C@H]1C(=O)N([C@H](C(=O)N([C@H](C(=O)NCCC(=O)O[C@@H](C(=O)N2CCC[C@H]2C(=O)N1)CC=C)C)C)C(C)C)C
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| InChi Key |
XIYSEKITPHTMJT-OCCJOITDSA-N
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| InChi Code |
InChI=1S/C29H47N5O7/c1-9-12-21-27(38)34-16-11-13-20(34)26(37)31-23(18(5)10-2)28(39)33(8)24(17(3)4)29(40)32(7)19(6)25(36)30-15-14-22(35)41-21/h9,17-21,23-24H,1,10-16H2,2-8H3,(H,30,36)(H,31,37)/t18-,19-,20-,21+,23-,24-/m0/s1
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| Chemical Name |
(3R,10S,13S,16S,19S)-16-[(2S)-butan-2-yl]-10,11,14-trimethyl-13-propan-2-yl-3-prop-2-enyl-4-oxa-1,8,11,14,17-pentazabicyclo[17.3.0]docosane-2,5,9,12,15,18-hexone
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 1.7310 mL | 8.6549 mL | 17.3097 mL | |
| 5 mM | 0.3462 mL | 1.7310 mL | 3.4619 mL | |
| 10 mM | 0.1731 mL | 0.8655 mL | 1.7310 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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