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

Paprotrain 

Cat. No.: HY-101298 Purity: 99.54%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 84 In-stock
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25 mg USD 144 In-stock
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50 mg USD 228 In-stock
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100 mg USD 408 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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[4]

MKLP-2

1.35 μM (IC50)

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].

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

Molecular Weight

245.28

Formula

C₁₆H₁₁N₃

CAS No.

57046-73-8

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)

*"≥" 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
10 mM 0.4077 mL 2.0385 mL 4.0770 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: ≥ 2.5 mg/mL (10.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

PaprotrainKinesinInhibitorinhibitorinhibit

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Paprotrain
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