WZ4003
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Molecular Weight (MW) | 496.99 |
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Formula |
C25H29ClN6O3 |
CAS No. | 1214265-58-3 |
Synonyms | N/A |
Solubility (25°C) | |
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Storage | 2 years -20℃Powder |
6 months-80℃in DMSO |
Chemical Name | Propanamide, N-?[3-?[[5-?chloro-?2-?[[2-?methoxy-?4-?(4-?methyl-?1-?piperazinyl)?phenyl]?amino]?-?4-?pyrimidinyl]?oxy]?phenyl]?- |
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Description | WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively, without significant inhibition on 139 other kinases. | |||||
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Targets | NUAK1 | NUAK2 | ||||
IC50 | 20 nM | 100 nM [1] | ||||
In vitro | In HEK-293 cells expressing wild-type NUAK1, WZ4003 (3–10 μM) markedly suppresses NUAK1-mediated MYPT1 phosphorylation. Moreover, WZ4003 (10 μM) inhibits MYPT1 Ser445 phosphorylation as well as cell migration, invasion and proliferation to a similar extent as knock out in MEFs or knock down in U2OS cells of NUAK1. [1] WZ4003 also exhibits a high, specific affinity to the L858R/T790M mutant EGFR, while a significantly reduced cellular IC50 against T790M containing Ba/F3 cells. [2] | |||||
In vivo | ||||||
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