WZ4003
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
WZ4003是有效的NUAK1和NUAK2选择性抑制剂,其IC50值分别为20 nM和100 nM[1].
NUAK家族SNF1样激酶1(NUAK1)与相关的NUAK2属于AMP活化蛋白激酶(AMPK)家族,由肿瘤抑制蛋白激酶肝激酶B1(LKB1)激活[1].
WZ4003是一种有效的和选择性的NUAK1/2抑制剂.在HEK-293细胞中,NUAK1可磷酸化肌球蛋白磷酸酶靶亚基1(MYPT1)的第445位丝氨酸,而WZ4003抑制MYPT1的磷酸化.在过表达NUAK1[A195T](抑制剂耐受型)的HEK293细胞中,WZ4003不抑制MYPT1在第445位丝氨酸的磷酸化.在小鼠胚胎成纤维细胞(MEFs)中,WZ4003显著抑制伤口愈合试验中的细胞迁移,并抑制MEF增殖.在细胞侵袭实验中,WZ4003抑制U2OS细胞的侵袭能力[1].在U2OS细胞中,WZ4003(10 μM)抑制MYPT1磷酸化并减少处于S期的细胞(50%).此外,WZ4003阻止细胞进入有丝分裂期[2].
参考文献：
[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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 496.99 |
| Cas No. | 1214265-58-3 |
| Formula | C25H29ClN6O3 |
| Solubility | insoluble in H2O; ≥2.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥7.85 mg/mL in DMSO with gentle warming |
| Chemical Name | N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide |
| SDF | Download SDF |
| Canonical SMILES | CCC(=O)NC1=CC(=CC=C1)OC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 酶学实验[1]: | |
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激酶检测 |
使用Cerenkov，通过定量Sakamototide底物肽中来自于[γ-32P]ATP的放射性32P的数量来测量纯化的GST-NUAK1的体外活性。反应在30℃、50μl反应体积进行30分钟，通过将40μl反应混合物点样到P81纸上并立即浸入50mM正磷酸中终止反应。样品在50mM正磷酸中洗涤三次，随后用丙酮冲洗一次，空气干燥。通过Cerenkov计数定量激酶介导的从[γ-32P]ATP中掺入Sakamototide底物肽的32P。 |
| 细胞实验[1]: | |
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细胞系 |
U2OS细胞系 |
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溶解方法 |
在DMSO中的溶解度> 7.85mg/mL。为了获得更高浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
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反应条件 |
10 μM作用16小时 |
|
应用 |
WZ4003在3D细胞侵袭试验中降低了U2OS细胞的侵袭潜力，效果与NUAK1敲低相同，这表明WZ4003可作为阐述NUAK激酶生物学作用的化学探针。 |
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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. |
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质量控制和MSDS
- 批次:
化学结构
