(5Z)-7-Oxozeaenol
(Synonyms: FR148083,L-783,279,LL-Z 1640-2) 目录号 : GC13944A selective TAK1 inhibitor
Cas No.:66018-38-0,253863-19-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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]. |
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. |
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.
Cas No. | 66018-38-0,253863-19-3 | SDF | |
别名 | FR148083,L-783,279,LL-Z 1640-2 | ||
化学名 | (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 | ||
分子式 | C19H22O7 | 分子量 | 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 | 储存条件 | Desiccate at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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