Brief Description

WZ4003 is a first potent and highly specific protein kinase inhibitor of NUAK kinases with IC50 of 20 nM/100 nM for NUAK1/NUAK2; no significant inhibition on 139 other kinases.
IC50 value: 20 nM/100 nM(NUAK1/2)
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). We also identify a mutation (A195T) that does not affect basal NUAK1 activity, but renders it ~50-fold resistant to both WZ4003 and HTH-01-015. Administration of WZ4003 and HTH-01-015 to MEFs (mouse embryonic fibroblasts) 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 and U2OS cells to the same extent as NUAK1 shRNA knockdown.

Solubility

DMSO

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Storage conditions

Store at -20°C 2 years

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