tcsc3258 WZ4003

WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC₅₀ of 20 nM/100 nM for NUAK1/NUAK2, without significant inhibition on other 139 kinases.

IC50 & Target: IC50: 20 nM (NUAK1), 100 nM (NUAK2)

In Vitro: WZ4003 (3-10 μM) markedly suppresses NUAK1-mediated MYPT1 phosphorylation, in HEK-293 cells expressing wild-type NUAK1. 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].