Poloxin

SKU: orb1218169

Description

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor. It targets the polo-box domain (IC50: appr 4.8 μM).

Key Properties

• CAS Number: 321688-88-4
• MW: 297.35
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉NO₃
• SMILES: CC(C)C(C(C=C1C)=O)=C/C1=N/OC(c1c(C)cccc1)=O
• Target: PLK
• Solubility: DMSO:14 mg/mL (43.72 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231.
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• In Vitro:
  Poloxin (25 μM) induces 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 inhibits proliferation in both cell lines with a comparable efficiency through 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC50 of ~4.8 μM. Poloxin exhibits 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: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PLK