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Poloxin PLK inhibitor

Cat.No.S5893

Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. This compound'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 PLK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 297.35

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (198.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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 add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 297.35 Formula

C18H19NO3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 321688-88-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)C1=CC(=N/OC(=O)C2=CC=CC=C2C)/C(=CC1=O)C

Mechanism of Action

Targets/IC50/Ki
Plk1 PBD
(in fluorescence polarization assays)
4.8 μM
In vitro

This compound 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.
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.
References

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