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Poloxin

Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. Poloxin's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays.

Poloxin Chemical Structure

Poloxin Chemical Structure

CAS No. 321688-88-4

Purity & Quality Control

Batch: S589301 DMSO]59 mg/mL]false]Ethanol]30 mg/mL]false]Water]Insoluble]false Purity: 99.41%
99.41

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Signaling Pathway

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PLK Signaling Pathway

Biological Activity

Description Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. Poloxin's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays.
Targets
Plk1 PBD [1]
(in fluorescence polarization assays)
4.8 μM
In vitro
In vitro

Poloxin is a small-molecule inhibitor specifically targeting the function of the polo-box domain (PBD) of Polo-like kinase 1 (Plk1), which strongly inhibits proliferation of cancer cells by inducing mitotic arrest, followed by a surge of apoptosis.[2]
Cell Research Cell lines HeLa cells
Concentrations 25 µM
Incubation Time 10 h
Method

HeLa cells are synchronized with double thymidine block and released into fresh medium with either DMSO or 25 µM Poloxin for 10 hours. Cells are fixed and stained for α-tubulin, pericentrin, and DNA. The morphological features of centrosomes, spindles, and chromosomes are examined by fluorescence microscopy.
In Vivo
In vivo

Poloxin significantly suppresses tumor growth of cancer cell lines in xenograft mouse models by lowering the proliferation rate and triggering apoptosis in treated tumor tissues.[2]

Chemical Information & Solubility

Molecular Weight 297.35 Formula

C18H19NO3
CAS No. 321688-88-4 SDF --
Smiles CC(C)C1=CC(=N/OC(=O)C2=CC=CC=C2C)/C(=CC1=O)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 59 mg/mL ( (198.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble


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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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