WZ4003 is a highly specific inhibitor of NUAK kinase, and the IC50 of NUAK1 and NUAK2 was 20 nM and 100 nM, respectively, with no significant inhibition on other 139 kinases.

 

Brand: BCM

 

Target: AMPK

 

Signaling Pathways: Chromatin/Epigenetic; PI3K/Akt/mTOR signaling

 

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.

 

pKa: 14.27±0.70(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: CCC(=O)NC1=CC(=CC=C1)OC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC  

 

InChIKey: SDGJBAUIGHSMRI-UHFFFAOYSA-N  

InChI: InChI=1S/C25H29ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h5-9,14-16H,4,10-13H2,1-3H3,(H,28,33)(H,27,29,30) 

 

Attribute
[Chem Name]	N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
[Synonym]	WZ4003
[CAS No.]	1214265-58-3
[MDL No.]	MFCD28015100
[Formula]	C25H29ClN6O3
[Molecular]	496.99
[Form]	White to beige powder
[Storage]	Keep in dark place. Inert atmosphere. Store in freezer, under -20°C

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