2. Cell Cycle/DNA Damage Cytoskeleton
  3. Kinesin
  4. Paprotrain

Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.

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

Paprotrain Chemical Structure

Paprotrain Chemical Structure

CAS No. : 57046-73-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 70 In-stock
25 mg USD 120 In-stock
50 mg USD 210 In-stock
100 mg USD 320 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Paprotrain Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Paprotrain

View All Kinesin Isoform Specific Products:

View All Isoforms
Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.

IC50 & Target

MKLP-2

1.35 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 GI50
> 50 μM
Compound: 1
Growth inhibition of human A549 cells incubated for 4 days by WST-1 assay
Growth inhibition of human A549 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
HCT-116 GI50
> 50 μM
Compound: 1
Growth inhibition of human HCT116 cells incubated for 4 days by WST-1 assay
Growth inhibition of human HCT116 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
HepG2 GI50
> 50 μM
Compound: 1
Growth inhibition of human HepG2 cells incubated for 4 days by WST-1 assay
Growth inhibition of human HepG2 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
HT-29 GI50
> 50 μM
Compound: 1
Growth inhibition of human HT-29 cells incubated for 4 days by WST-1 assay
Growth inhibition of human HT-29 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
K562 GI50
21.6 μM
Compound: 1
Growth inhibition of human K562 cells incubated for 4 days by WST-1 assay
Growth inhibition of human K562 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
MCF7 GI50
> 50 μM
Compound: 1
Growth inhibition of human MCF7 cells incubated for 4 days by WST-1 assay
Growth inhibition of human MCF7 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
MDA-MB-231 GI50
> 50 μM
Compound: 1
Growth inhibition of human MDA-MB-231 cells incubated for 4 days by WST-1 assay
Growth inhibition of human MDA-MB-231 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
MIA PaCa-2 GI50
> 50 μM
Compound: 1
Growth inhibition of human MIAPaCa2 cells incubated for 4 days by WST-1 assay
Growth inhibition of human MIAPaCa2 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
NCI-H460 GI50
> 50 μM
Compound: 1
Growth inhibition of human NCI-H460 cells incubated for 4 days by WST-1 assay
Growth inhibition of human NCI-H460 cells incubated for 4 days by WST-1 assay
[PMID: 26778612]
In Vitro

Paprotrain has been screened on a panel of CNS kinases. While inactive (IC50 >10 μM) on CDK5 and GSK3, it has shown a moderate activity on DYRK1A (IC50=5.5 μM)[1]. Time-lapse microscopy shows that disrupting MKlp2 expression with paprotrain results in polar body extrusion failure. This could be rescued after rescuing oocytes from paprotrain in fresh medium. Cell cycle analysis shows that most oocytes are arrested at metaphase I or telophase I. However, oocyte spindle structure and chromosome alignment are not disrupted after the inhibition of MKlp2 by paprotrain[2]. Paprotrain-treated porcine oocytes suffer failure of nuclear maturation. The number of oocytes arrested at early MI stage increase in a dose-dependent manner after KIF20A activity inhibition, while the percentage of oocytes that reach ATI and MII stages decrease after treatment[3].

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

Paprotrain Related Antibodies
Molecular Weight

245.28

Formula

C16H11N3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#C/C(C1=CNC2=CC=CC=C21)=C\C3=CN=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (407.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0770 mL 20.3849 mL 40.7697 mL
5 mM 0.8154 mL 4.0770 mL 8.1539 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 2.5 mg/mL (10.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

Purity: 99.87%

SDS (393 KB)

COA (246 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Kinase activities for each enzyme are assayed in the presence of 15 μM ATP in a final volume of 30 μL. After 30 min incubation at 30°C, the reaction is stopped by harvesting, using a FilterMate harvester, onto P81 phosphocellulose papers which are washed in 1% phosphoric acid. 20 μL of scintillation fluid are added and the incorporated radioactivity measured in a Packard counter. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated during the 30 min incubation. Controls are performed with appropriate dilutions of DMSO. Kinase activities are expressed in % of maximal activity, i.e. in the absence of inhibitors (Paprotrain). IC50 values are obtained from the dose-response curves[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[3]

COCs or denuded oocytes (DOs) are cultured in the presence/absence of Paprotrain in vitro. The control groups are performed with pure DMSO at the same concentration. COCs are denuded of their cumulus cells by gentle pipetting with 0.1% (w/v) hyaluronidase. Oocytes with clearly extruded polar bodies are judged to be matured oocytes. After cultured for 44 h, the polar body extrusion rate of matured oocytes is observed using a microscope. Furthermore, chromosomal alignments and the cell cycle of oocytes treated with inhibitor are examined using laser scan confocal microscopy[3].

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0770 mL 20.3849 mL 40.7697 mL 101.9243 mL
5 mM 0.8154 mL 4.0770 mL 8.1539 mL 20.3849 mL
10 mM 0.4077 mL 2.0385 mL 4.0770 mL 10.1924 mL
15 mM 0.2718 mL 1.3590 mL 2.7180 mL 6.7950 mL
20 mM 0.2038 mL 1.0192 mL 2.0385 mL 5.0962 mL
25 mM 0.1631 mL 0.8154 mL 1.6308 mL 4.0770 mL
30 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3975 mL
40 mM 0.1019 mL 0.5096 mL 1.0192 mL 2.5481 mL
50 mM 0.0815 mL 0.4077 mL 0.8154 mL 2.0385 mL
60 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
80 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2741 mL
100 mM 0.0408 mL 0.2038 mL 0.4077 mL 1.0192 mL
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Paprotrain 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:

Paprotrain57046-73-8KinesinInhibitorinhibitorinhibit

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