NSC668394

SKU: orb1699797

Description

NSC668394 is a potent inhibitor of ezrin phosphorylation at Thr567, which suppresses its role in tumor metastasis. Its mechanism involves promoting Ca2+-dependent ezrin cleavage, demonstrating antitumor potential in cellular studies. This compound is a valuable tool for investigating cancer cell motility and invasion in vitro.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 382605-72-3
• MW: 452.1
• Purity: 99.29% (May vary between batches)
• Formula: C₁₇H₁₂Br₂N₂O₃
• SMILES: Oc1c(Br)cc(CCNC2=CC(=O)c3cccnc3C2=O)cc1Br
• Target: PKC
• Solubility: DMSO:30 mg/mL (66.36 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.42 mM)

Bioactivity

• Target IC50:
  Ezrin T567:8.1 μM
• In Vivo:
  Administered at a dose of 0.226 mg/kg/day through weekly intraperitoneal injections for 5 days, NSC668394 inhibits ezrin protein-dependent in vivo metastatic growth in the lungs of mice.
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• In Vitro:
  NSC668394, when pretreated at 10 μM for 15 minutes, inhibits ezrin T567 phosphorylation (IC50=8.1 μM) and in vitro actin binding. Additionally, at concentrations ranging from 1 to 10 μM for 2 to 6 hours, NSC668394 inhibits ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells into HUVEC monolayers. Furthermore, at a concentration of 20 μM, NSC668394 significantly reduces the growth of JM1 and JM2 rat hepatocellular carcinoma cell lines. Notably, NSC668394 at 10 μM diminishes cell motility phenotypes in zebrafish.
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Storage & Handling

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

Alternative Names

NSC668394, NSC-668394, NSC 668394, PKC

Compound Identifiers

PubChem CID

381594