Paprotrain (Synonyms: Passenger Proteins Transport Inhibitor) |
| Catalog No.GC12788 |
mitotic kinesin-like protein 2 (MKLP-2) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 57046-73-8
Sample solution is provided at 25 µL, 10mM.
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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.
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].
Reference:
[1]. Labrière C, et al. Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. Eur J Med Chem. 2016 Nov 29;124:920-934.
[2]. Liu J, et al. MKlp2 inhibitor paprotrain affects polar body extrusion during mouse oocyte maturation. Reprod Biol Endocrinol. 2013 Dec 21;11:117.
[3]. Zhang Y, et al. KIF20A regulates porcine oocyte maturation and early embryo development.
[4]. Tcherniuk S, et al. Relocation of Aurora B and survivin from centromeres to the central spindle impaired by a kinesin-specific MKLP-2 inhibitor. Angew Chem Int Ed Engl. 2010 Oct 25;49(44):8228-31.
Kinase experiment: | 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]. |
Cell experiment: | 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]. |
References: [1]. Labrière C, et al. Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. Eur J Med Chem. 2016 Nov 29;124:920-934. | |
| Cas No. | 57046-73-8 | SDF | |
| Synonyms | Passenger Proteins Transport Inhibitor | ||
| Chemical Name | (Z)-2-(1H-indol-3-yl)-3-(pyridin-3-yl)acrylonitrile | ||
| Canonical SMILES | N#C/C(C1=CNC2=CC=CC=C12)=C([H])\C3=CN=CC=C3 | ||
| Formula | C16H11N3 | M.Wt | 245.28 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.1 mg/ml,Ethanol: 0.2 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.077 mL | 20.3849 mL | 40.7697 mL |
| 5 mM | 0.8154 mL | 4.077 mL | 8.1539 mL |
| 10 mM | 0.4077 mL | 2.0385 mL | 4.077 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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