[CAS NO. 1214265-58-3] WZ4003

Name: WZ4003
Brand: Arctom Scientific
SKU: SLK-S7317

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PRODUCTS SPECIFICATIONS [1214265-58-3]

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Catalog

SLK-S7317

Brand

Selleck

CAS

1214265-58-3

DESCRIPTION [1214265-58-3]

Overview

MDL	MFCD28015100
Molecular Weight	496.99
Molecular Formula	C25H29ClN6O3
SMILES	O(C)C=1C=C(C=CC1NC=2N=C(OC3=CC(NC(CC)=O)=CC=C3)C(Cl)=CN2)N4CCN(C)CC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0121 mL	10.0606 mL	20.1211 mL
5 mM	0.4024 mL	2.0121 mL	4.0242 mL
10 mM	0.2012 mL	1.0061 mL	2.0121 mL
50 mM	-	-	-

Description

WZ4003 is a highly specific inhibitor with of 20 nM and 100 nM for NUAK1 and NUAK2 in cell-base assays, respectively, without significant inhibition on 139 other kinases.

Targets

NUAK1 ^[1] (Cell-free assay)	NUAK2 ^[1] (Cell-free assay)
20 nM	100 nM

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. 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.

References

[1] Banerjee S, et al. Biochem J. 2014, 457(1), 215-225.
[2] Zhou W, et al. Nature. 2009, 462(7276), 1070-1074.

Synonyms

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

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