WZ 4003

Modify Date: 2024-01-02 18:10:41

WZ 4003 structure	Common Name	WZ 4003
	CAS Number	1214265-58-3	Molecular Weight	496.989
	Density	1.3±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₂₅H₂₉ClN₆O₃	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A
	Symbol	GHS07	Signal Word	Warning

Use of WZ 4003

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.

Name	N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
Synonym	More Synonyms

Description	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.
Related Catalog	Signaling Pathways >> Epigenetics >> AMPK Signaling Pathways >> PI3K/Akt/mTOR >> AMPK Research Areas >> Cancer
Target	NUAK1:20 nM (IC50) NUAK2:100 nM (IC50)
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].
Kinase Assay	In vitro activities of purified GST-NUAK1 and GST-NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalysed the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h.
Cell Assay	Cell proliferation assays are carried out colorimetrically in 96-well plates. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015 or WZ4003.
References	[1]. Banerjee S, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. [2]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.

Density	1.3±0.1 g/cm3
Molecular Formula	C₂₅H₂₉ClN₆O₃
Molecular Weight	496.989
Exact Mass	496.198975
PSA	95.34000
LogP	3.50
Index of Refraction	1.639
Storage condition	-20℃

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Precautionary Statements	P301 + P312 + P330
Hazard Codes	Xn
RIDADR	NONH for all modes of transport

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

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

WZ4003

DC Chemicals Limited
China
Product Name: WZ-4003
Price: $300.0/100mg $500.0/250mg $1000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: $103/10mM*1mLinDMSO

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WZ 4003

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