WZ4003

SKU: orb1300897

Description

WZ4003 is a potent and selective NUAK kinase inhibitor, exhibiting IC50 values of 20 nM for NUAK1 and 100 nM for NUAK2 with minimal off-target activity against 139 other kinases. This tool compound is widely used in vitro and in vivo to investigate the roles of NUAK1/2 in cancer biology, cell metabolism, and autophagy.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1214265-58-3
• MW: 496.99
• Purity: >99.99% (May vary between batches)
• Formula: C₂₅H₂₉ClN₆O₃
• SMILES: CCC(=O)Nc1cccc(Oc2nc(Nc3ccc(cc3OC)N3CCN(C)CC3)ncc2Cl)c1
• Target: AMPK
• Solubility: DMSO:8 mg/mL (16.1 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  NUAK2:100 nM|NUAK1:20 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.
• Cell Research:
  Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. 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 WZ4003.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NUAK1, NUAK2, inhibit, Inhibitor, AMPK, AMP-activated protein kinase, WZ 4003, WZ4003, WZ-4003

Compound Identifiers

PubChem CID

72200024