WZ4003

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WZ4003 是一种高度特异性的 NUAK 激酶抑制剂，对 NUAK1 和 NUAK2 的 IC50 分别为 20 nM 和 100 nM。

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.

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. 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.

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WZ4003 | WZ-4003 | WZ 4003

Membrane Transporter/Ion Channel

AMPK

NUAK1| NUAK2

Cancer

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1214265-58-3

496.99

C25H29ClN6O3

>98% (HPLC)

DMSO:7 mg/mL (14.08 mM); Ethanol:<1 mg/mL (<1 mM); Water：<1 mg/mL (<1 mM)

CCC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O

N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide

(-20℃)

With Ice Pack

≥ 2 years