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Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $350 | In Stock | |
5 mg | $970 | In Stock | |
10 mg | $1,200 | In Stock | |
25 mg | $1,590 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,500 | In Stock | |
500 mg | $4,910 | In Stock |
Description | Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells. |
Targets&IC50 | NPCs:1 μM |
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[2].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[1]. |
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[1]. |
Alias | Poloxin2, Poloxin 2 |
Molecular Weight | 269.3 |
Formula | C16H15NO3 |
Cas No. | 321695-37-8 |
Smiles | N(OC(=O)C1=C(C)C=CC=C1)=C2C(C)=CC(=O)C(C)=C2 |
Relative Density. | 1.13 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 12.5 mg/mL (46.4 mM), Sonification is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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