Poloxin

SKU: orb1307861

Description

Poloxin

Research Area

Cell Biology

Key Properties

• CAS Number: 321688-88-4
• MW: 297.35
• Purity: 96.62% (May vary between batches)
• Formula: C₁₈H₁₉NO₃
• SMILES: CC(C)C1=C\C(=N\OC(=O)c2ccccc2C)C(C)=CC1=O
• Target: PLK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.36 mM);DMSO:14 mg/mL (47.08 mM)

Bioactivity

• Target IC50:
  PLK3 (PBD):53.9 μM|PLK1 (PBD):4.8 μM|PLK2 (PBD):18.7 μM
• In Vivo:
  Poloxin (40 mg/kg) reduces the proliferation of MDA-MB-231 cells. It also suppresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231.
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• In Vitro:
  Poloxin inhibits proliferation in both cell lines with a comparable efficiency through a 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction (apparent IC50: ～4.8 μM). Poloxin (25 μM) causes defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin shows a loose Plk1 PBD specificity with 4-10 times higher IC50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains.
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Storage & Handling

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

Alternative Names

Inhibitor, PLK2, PLK1 PBD, PLK2 PBD, PLK3, PLK3 PBD, PLK1, PLK, inhibit, Poloxin, Polo-like Kinase (PLK)

Compound Identifiers

PubChem CID

9613592