1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)
  3. Poloxin

Poloxin 

Cat. No.: HY-12134 Purity: 98.01%
COA Handling Instructions

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.

For research use only. We do not sell to patients.

Poloxin Chemical Structure

Poloxin Chemical Structure

CAS No. : 321688-88-4

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Solution
10 mM * 1 mL in DMSO USD 72 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 41 In-stock
10 mg USD 65 In-stock
50 mg USD 264 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.

IC50 & Target[4]

PLK1 PBD

4.8 μM (IC50)

PLK2 PBD

18.7 μM (IC50)

PLK3 PBD

53.9 μM (IC50)

In Vitro

Poloxin (25 μM) induces 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[1]. Poloxin inhibits proliferation in both cell lines with a comparable efficiency through 72 h period[2]. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC50 of ∼4.8 μM. Poloxin exhibits 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

297.35

Appearance

Solid

Formula

C18H19NO3

CAS No.
SMILES

O=C(C(C(C)C)=C/1)C=C(C)C1=N/OC(C2=CC=CC=C2C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 14.29 mg/mL (48.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3630 mL 16.8152 mL 33.6304 mL
5 mM 0.6726 mL 3.3630 mL 6.7261 mL
10 mM 0.3363 mL 1.6815 mL 3.3630 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.43 mg/mL (4.81 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.43 mg/mL (4.81 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
Cell Assay
[2]

Cell Viability Assay on treated cells in 96-well plates, based on viable cells. 20 μL of CellTiter-Blue®reagent is added to each well and then incubated at 37°C with 5% CO2 for 4h before fluorescence reading using a Victor 1420 Multilabel Counter. All experiments are performed in triplicate and at least three independent experiments are performed. Data are presented as percentage compared with control.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Viable MDA-MB-231 or HeLa cells (1×106) are resuspended in 300 μL of 0.9% NaCl and s.c. injected into both flanks of nude mice (MDA-MB-231: n=8 mice in each group, total N=16; HeLa: n=7 mice in each group, total N=14). Approximately 3 weeks after inoculation, mice are treated with Poloxin (40 mg/kg) or TQ (20 mg/kg) by intratumoral injection on Mondays, Wednesdays, and Fridays for 5 to 6 weeks. The tumor area is calculated by multiplication of the greatest diameter with the perpendicular diameter every 2 to 3 days. Measurements of all tumors within the group are represented by the mean value. U-tests and Student's t-tests are performed for statistical evaluation among MDA-MB-231 groups and between HeLa groups, respectively. All mice are properly treated in accordance with the guidelines of the local animal committee.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Poloxin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
Poloxin
Cat. No.:
HY-12134
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