WZ4003
目录号 : GC16549
A selective NUAK1 and NUAK2 inhibitor
Cas No.:1214265-58-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
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Kinase assays |
In vitro activities of purified GST–NUAK1 were measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions were carried out in a 50 μl reaction volume for 30 min at 30°C and reactions were terminated by spotting 40 μl of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples were washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide was quantified by Cerenkov counting. |
| Cell experiment [2]: | |
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Cell lines |
U2OS cell lines |
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Preparation method |
The solubility of this compound in DMSO is >7.85mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
10 μM for 16h |
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Applications |
WZ4003 impaired the invasive potential of U2OS cells in a 3D cell invasion assay to the same extent as NUAK1 knockdown, which indicates that WZ4003 will serve as useful chemical probes to delineate the biological roles of the NUAK kinases. |
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References: [1] Banerjee S, Buhrlage SJ, Huang HT, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J, 2014, 457(1): 215-225. | |
WZ4003 is a potent and selective inhibitor of NUAK1 and NUAK2 with IC50 values of 20 and 100 nM, respectively [1].
NUAK family SNF1-like kinase-1 (NUAK1) and the related NUAK2 belong to the AMP-activated protein kinase (AMPK) family and are activated by liver kinase B1 (LKB1) tumour suppressor protein kinase [1].
WZ4003 is a potent and selective NUAK1/2 inhibitor. In HEK-293 cells, WZ4003 inhibited the phosphorylation of myosin phosphate-targeting subunit 1 (MYPT1), which was phosphorylated by NUAK1 at Ser445. In HEK-293 cells overexpressing inhibitor-resistant NUAK1[A195T], WZ4003 didn’t inhibit the phosphorylation of MYPT1 at Ser445. In mouse embryonic fibroblasts (MEFs), WZ4003 significantly inhibited migration in a wound-healing assay and inhibited MEFs proliferation. In a cell invasion assay, WZ4003 inhibited the invasive potential of U2OS cells [1]. In U2OS cells, WZ4003 (10 μM) inhibited phosphorylation of MYPT1 and reduced the cells in S-phase by 50%. Also, WZ4003 prevented cells from entering into mitosis [2].
References:
[1]. Banerjee S, Buhrlage SJ, Huang HT, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J, 2014, 457(1): 215-225.
[2]. Banerjee S, Zagórska A, Deak M, et al. Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase. Biochem J, 2014, 461(2): 233-245.
| Cas No. | 1214265-58-3 | SDF | |
| 化学名 | N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide | ||
| Canonical SMILES | CCC(=O)NC1=CC(=CC=C1)OC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC | ||
| 分子式 | C25H29ClN6O3 | 分子量 | 496.99 |
| 溶解度 | ≥ 7.85mg/mL in DMSO with gentle warming | 储存条件 | Store 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0121 mL | 10.0606 mL | 20.1211 mL |
| 5 mM | 0.4024 mL | 2.0121 mL | 4.0242 mL |
| 10 mM | 0.2012 mL | 1.0061 mL | 2.0121 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。