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Poloxin-2

Catalog No. T25969   CAS 321695-37-8
Synonyms: Poloxin2, Poloxin 2

Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.

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Poloxin-2 Chemical Structure
Poloxin-2, CAS 321695-37-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 350.00
5 mg In stock $ 970.00
10 mg In stock $ 1,200.00
25 mg In stock $ 1,590.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,500.00
500 mg In stock $ 4,910.00
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Purity: 99.59%
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Biological Description
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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].
Synonyms Poloxin2, Poloxin 2
Molecular Weight 269.3
Formula C16H15NO3
CAS No. 321695-37-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Polson ES, et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018 Aug 15;10(454). pii: eaar2718. 2. Wurdak H, et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc Natl Acad Sci U S A. 2010 Sep 21;107(38):16542-7.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library

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Keywords

Poloxin-2 321695-37-8 Cell Cycle/Checkpoint PLK Poloxin2 Poloxin 2 inhibitor inhibit

 

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