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Poloxin

Catalog No. T16560 CAS 321688-88-4

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

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Poloxin, CAS 321688-88-4

Pack Size	Availability	Price/USD
10 mg	In stock	$ 48.00
25 mg	In stock	$ 115.00
50 mg	In stock	$ 206.00
100 mg	In stock	$ 306.00
200 mg	In stock	$ 456.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.19%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor. It targets the polo-box domain (IC50: appr 4.8 μM).
Targets&IC50	PLK2 (PBD):18.7 μM, PLK1 (PBD):4.8 μM, PLK3 (PBD):53.9 μM
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[1][2][3].
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[1].

Molecular Weight	297.35
Formula	C18H19NO3
CAS No.	321688-88-4

Storage

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

Solubility Information

DMSO: 14 mg/mL (43.72 mM), Sonication is recommended.

References and Literature

1. Yuan J, et al. Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo. Am J Pathol. 2011 Oct;179(4):2091-9. 2. Sanhaji M, et al. p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors. Cell Cycle. 2012 Feb 1;11(3):543-53. 3. Lee KS, et al. Pinning down the polo-box domain. Chem Biol. 2008 May;15(5):415-6. 4. Reindl W, et al. Inhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions. Chem Biol. 2008 May;15(5):459-66.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Anti-Cancer Compound Library Cell Cycle Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Poloxin 321688-88-4 Cell Cycle/Checkpoint PLK Inhibitor Polo-like Kinase (PLK) inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.