WZ4003

SKU: orb1226780

Description

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.

Key Properties

• CAS Number: 1214265-58-3
• MW: 496.99
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₉ClN₆O₃
• SMILES: CCC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O
• Target: AMPK
• Solubility: DMSO:7 mg/mL (14.08 mM); Ethanol:<1 mg/mL (<1 mM); Water：<1 mg/mL (<1 mM)

Bioactivity

• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WZ4003 | WZ-4003 | WZ 4003

Quick Database Links

Gene Symbol

AMPK