Poloxin-2

SKU: orb1701781

Description

Poloxin-2 is a potent and selective inhibitor targeting the Polo-box domain (PBD) of Polo-like kinase 1 (Plk1). It demonstrates anti-tumor activity by reducing Plk1 protein levels in HeLa cells and has been utilized in vitro to study mitosis, cell cycle progression, and cancer therapeutics.

Research Area

Cell Biology

Key Properties

• CAS Number: 321695-37-8
• MW: 269.3
• Purity: 99.59% (May vary between batches)
• Formula: C₁₆H₁₅NO₃
• SMILES: N(OC(=O)C1=C(C)C=CC=C1)=C2C(C)=CC(=O)C(C)=C2
• Target: PLK
• Solubility: DMSO:12.5 mg/mL (46.42 mM)

Bioactivity

• Target IC50:
  NPCs:1 μM
• In Vivo:
  In tumors treated with Poloxin-2, there is a significant reduction in tumor cell proliferation (approximately two-fold decrease). Compared to tumors treated with the carrier control, Poloxin-2-treated tumors show signs of increased cell death (reduced cell structures/increased condensation). Poloxin-2treatment markedly reduces the expansion of frontal-to-tail tumor growth and corpus callosum invasion in waveform protein-positive GBM1 cells. It was also observed that the survival rate of animals carrying GBMX1 tumors (established 2 or 6 weeks prior to treatment) significantly increases with the 10-week Poloxin-2treatment regimen. No mouse had to be removed from the study due to adverse effects of the treatment. Another experiment using continuous Poloxin-2 treatment until the endpoint also shows a significant increase in the survival rate of animals carrying GBMX1 tumors. Histopathological endpoint analysis of animals treated with Poloxin-2 and the vehicle confirms a significant reduction in tumor size in Poloxin-2-treated mice.
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• In Vitro:
  Poloxin-2 increases neurite differentiation of rat NPCs in a dose-dependent manner (EC50=~1 μM) in adherent culture. Under neural sphere-forming conditions, Poloxin-2 (1.5-5 μM) induces neuronal formation in secondary neurospheres derived from adult rat hippocampus and subventricular zone (SVZ) (40-60% TuJ1+ cells).Furthermore, hippocampal NPCs treated with Poloxin-2and cultured on microelectrode arrays for 12 days exhibit neuronal morphology and spontaneous spike activity, indicating the presence of functional, mature neurons.In comparison to cells treated with the carrier (dimethyl sulfoxide, DMSO),Poloxin-2 significantly attenuates the growth of tumor cells.TACC3 is a known target of Poloxin-2 in rodent neural progenitor cells. Poloxin-2 has been shown to induce instability in cells expressing TACC3, leading to a gradual reduction in endogenous TACC3 protein levels over time.
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Storage & Handling

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

Alternative Names

PLK1, Poloxin2, Poloxin-2, Poloxin 2

Compound Identifiers

PubChem CID

5209280