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

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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Customer Review

Based on 3 publication(s) in Google Scholar

Poloxin Related Antibodies

Top Publications Citing Use of Products

View All Polo-like Kinase (PLK) Isoform Specific Products:

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PLK1 PLK2 PLK3 PLK4

  • 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].

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

Poloxin Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

297.35

Formula

C18H19NO3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3630 mL 16.8152 mL 33.6304 mL 84.0760 mL
5 mM 0.6726 mL 3.3630 mL 6.7261 mL 16.8152 mL
10 mM 0.3363 mL 1.6815 mL 3.3630 mL 8.4076 mL
15 mM 0.2242 mL 1.1210 mL 2.2420 mL 5.6051 mL
20 mM 0.1682 mL 0.8408 mL 1.6815 mL 4.2038 mL
25 mM 0.1345 mL 0.6726 mL 1.3452 mL 3.3630 mL
30 mM 0.1121 mL 0.5605 mL 1.1210 mL 2.8025 mL
40 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1019 mL
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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.

Keywords:

Poloxin321688-88-4Polo-like Kinase (PLK)Inhibitorinhibitorinhibit

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