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WZ4003 CAS:1214265-58-3

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产品名称: WZ4003 CAS:1214265-58-3
产品型号: C16481
产品展商: Chembest
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简单介绍

Product Name: WZ4003 CAS No.: 1214265-58-3 Molecular Weight: 496.99 Molecular Formula: C25H29ClN6O3


WZ4003 CAS:1214265-58-3  的详细介绍

Product Name: WZ4003
CAS No.: 1214265-58-3
Molecular Weight: 496.99
Molecular Formula: C25H29ClN6O3
Purity : >98%

Biological Activity:
WZ4003 is a first potent and highly specific protein kinase inhibitor of NUAK kinases with IC50 of 20 nM/100nM for NUAK1/NUAK2; no significant inhibition on 139 other kinases. 
IC50 value: 20 nM/100 nM(NUAK1/2) [1] 
Target: NUAK inhibitor 
In all cell lines tested, WZ4003 and HTH-01-015 inhibit the phosphorylation of the only well-characterized
substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser(445). Wealso identify a mutation (A195T) that does not affect basal NUAK1 activity, but renders it ~50-fold resistant toboth WZ4003 and HTH-01-015. Administration of WZ4003 and HTH-01-015 to MEFs (mouse embryonicfibroblasts) significantly inhibits migration in a wound-healing assay to a similar extent as NUAK1-knockout.WZ4003 and HTH-01-015 also inhibit proliferation of MEFs to the same extent as NUAK1 knockout andU2OS cells to the...

 

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