(5Z)-7-Oxozeaenol (Synonyms: FR148083,L-783,279,LL-Z 1640-2) |
| カタログ番号GC13944 |
TAK1ミトゲン活性化プロテインキナーゼキナーゼ（MAPKKK）阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 66018-38-0,253863-19-3
Sample solution is provided at 25 µL, 10mM.
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5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
5Z-7-Oxozeaenol is a potent irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 (TAK1, IC50, 8.1 nM), less active on MEK1 (IC50, 411 nM). 5Z-7-Oxozeaenol prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase[1]. 5Z-7-Oxozeaenol is also an inhibitor of VEGF-R2, with an IC50 of 52 nM. 5Z-7-Oxozeaenol has inhibitory activity against VEGF-R3, FLT3, PDGFR-β, B-RAF VE and SRC, with IC50s of 110, 170, 340, 6300 and 6600 nM, respectively[2]. 5Z-7-Oxozeaenol inhibits JNK/p38 paythway, but it is not a direct inhibitor and is signal specific. 5Z-7-Oxozeaenol suppresses the PMA-induced AP-1 activity almost to the basal level in the KT cells, but has no effects on IL-1-induced NF-kB activity in the KK cells[3].
Reference:
[1]. Ninomiya-Tsuji J, et al. A resorcylic acid lactone, 5Z-7-oxozeaenol, prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase. J Biol Chem. 2003 May 16;278(20):18485-90.
[2]. Dakas PY, et al. Modular synthesis of radicicol A and related resorcylic acid lactones, potent kinase inhibitors. Angew Chem Int Ed Engl. 2007;46(36):6899-902.
[3]. Takehana K, et al. A radicicol-related macrocyclic nonaketide compound, antibiotic LL-Z1640-2, inhibits the JNK/p38 pathways in signal-specific manner. Biochem Biophys Res Commun. 1999 Apr 2;257(1):19-23.
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Kinase experiment: |
For screening TAK1 inhibitors, insect expression vectors for TAK1 and TAB1 are co-infected into Sf9 cells. After 2 days of incubation, cell lysates are immunoprecipitated with anti-TAK1 antibody (M-17). The immunoprecipitates are incubated with various compounds (5Z-7-Oxozeaenol, etc.) and subsequently incubated with 2 μg of myelin basic protein and 10 μCi of [γ-32P]ATP (3,000 Ci/mmol) in 10 μL of the kinase buffer containing 10 mM HEPES (pH 7.4), 1 mM dithiothreitol, 5 mM MgCl2 at 30°C for 5 min. Samples are separated by 10% SDS-PAGE, and 32P incorporated into myelin basic protein is quantified with a bioimage analyzer. The catalytic activity of MEK1 is determined by activation of ERK2 to phosphorylate dure. The catalytic activity of MEKK1 is measured with 2 μg of myelin basic protein as a substrate in the kinase buffer. For subsequent kinase assays, immunoprecipitates are incubated with 5 μCi of [γ-32P]ATP (3,000 Ci/mmol) and 1 μg of bacterially expressed MKK6 or GST-IκBα-(1-72) in 10 μL of the kinase buffer at 25°C for 2 min. Samples are separated by 10% SDS-PAGE and visualized by autoradiography[1]. |
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References: [1]. Ninomiya-Tsuji J, et al. A resorcylic acid lactone, 5Z-7-oxozeaenol, prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase. J Biol Chem. 2003 May 16;278(20):18485-90. |
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| Cas No. | 66018-38-0,253863-19-3 | SDF | |
| 同義語 | FR148083,L-783,279,LL-Z 1640-2 | ||
| Chemical Name | (3S,5Z,8S,9S,11E)-8,9,16-trihydroxy-14-methoxy-3-methyl-3,4,9,10-tetrahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione | ||
| Canonical SMILES | O[C@@H](C/C=C/C(C=C1OC)=C(C(O)=C1)C(O[C@@H](C)C/C=C\C2=O)=O)[C@@H]2O | ||
| Formula | C19H22O7 | M.Wt | 362.37 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:20): 50 µg/ml,Ethanol: 1 mg/ml | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7596 mL | 13.7981 mL | 27.5961 mL |
| 5 mM | 0.5519 mL | 2.7596 mL | 5.5192 mL |
| 10 mM | 0.276 mL | 1.3798 mL | 2.7596 mL |
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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