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WZ4003

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Chemical Structure| 1214265-58-3 同义名 : -
CAS号 : 1214265-58-3
货号 : A200517
分子式 : C25H29ClN6O3
纯度 : 98+%
分子量 : 496.989
MDL号 : MFCD28015100
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(70.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AMPK

    NUAK2, IC50:100 nM

    NUAK1, IC50:20 nM
描述 NUAK family SNF1-like kinase-1 (NUAK1) and NUAK2 are the members of the AMPK family that play important roles in regulating essential cellular events, such as cell invasion, proliferation, embryonic development and axon branching. WZ4003 is an inhibitor of both NUAK isoforms with IC50 values of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. In HEK-293 cells, EDTA-induced phosphorylation of MYPT1 at Ser445 was suppressed by WZ4003 (0.3 - 10 mM) in a dose-dependent manner. In HEK-293 cells expressing drug-resistant NUAK1[A195T], WZ4003 at 30 μM failed to block the phosphorylation of MYPT1. However, WZ4003 at 3 - 10 μM effectively suppressed MYPT1 Ser445 phosphorylation. Treatment with 10 μM WZ4003 remarkably reduced cell migration in wild-type mouse embryonic fibroblasts (MEFs). In both U2OS cells and MEFs, WZ4003 at 10 μM suppressed cell proliferation and MYPT1 phosphorylation to the same level as shown in NUAK1 knockout cells. The invasion potential of U2OS cells was also inhibited by 10 μM WZ4003[3]. In the Ba/F3 cell line, the IC50 values of WZ4003 against L858R/T790M mutant and T790M mutant were 1.90 mM and 1.29 mM, respectively[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.06mL

2.01mL

1.01mL

20.12mL

4.02mL

2.01mL
参考文献

[1]Banerjee S, Buhrlage SJ, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.

[2]Zhou W, Ercan D, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.

[3]Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PMID: 24171924; PMCID: PMC3969223.

[4]Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622. PMID: 20033049; PMCID: PMC2879581.