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Submit ReviewWZ 4003 is a potent and selective NUAK1/2 inhibitor (IC50 values are 20 and 100 nM respectively). Exhibits no significant inhibition against a panel of 139 kinases, including ten AMPK family members. Inhibits NUAK1-mediated MYPT1 phosphorylation. Also inhibits cell proliferation in U2OS cells.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of WZ 4003 is reviewed on the chemical probes website.
分子量 | 496.99 |
公式 | C25H29ClN6O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1214265-58-3 |
PubChem ID | 72200024 |
InChI Key | SDGJBAUIGHSMRI-UHFFFAOYSA-N |
Smiles | CN(CC3)CCN3C(C=C2)=CC(OC)=C2NC1=NC=C(Cl)C(OC4=CC(NC(CC)=O)=CC=C4)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
1eq. HCl | 24.85 | 50 | |
DMSO | 9.94 | 20 温和加热 |
以下数据基于产品分子量 496.99。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.02 mL | 20.12 mL | 40.24 mL |
2.5 mM | 0.8 mL | 4.02 mL | 8.05 mL |
5 mM | 0.4 mL | 2.01 mL | 4.02 mL |
25 mM | 0.08 mL | 0.4 mL | 0.8 mL |
参考文献是支持产品生物活性的出版物。
Zhou et al (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462 1070 PMID: 20033049
Banerjee et al (2014) Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase. Biochem.J. 461 233 PMID: 24785407
Banerjee et al (2014) Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem.J. 457 215 PMID: 24171924
If you know of a relevant reference for WZ 4003, please let us know.
关键词: WZ 4003, WZ 4003 supplier, WZ4003, potent, selective, NUAK1, inhibitors, inhibits, NUAK2, NUAK, MYPT1, kinases, 5177, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 WZ 4003 的部分引用包括:
Sebastian et al (2019) Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chem Biol 26 1703-1715.e37 PMID: 31676236
Raymond S et al (2020) Pharmacoproteomics Identifies Kinase Pathways that Drive the Epithelial-Mesenchymal Transition and Drug Resistance in Hepatocellular Carcinoma. Cell Syst 11 196-207.e7 PMID: 32755597
Anne-Claude et al (2020) A novel role for NUAK1 in promoting ovarian cancer metastasis through regulation of fibronectin production in spheroids. Cancers (Basel) 12 PMID: 32429240
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.