Paprotrain
Based on 5 publication(s) in Google Scholar
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.
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- Pureté: 99.85%
- CAS No.: 57046-73-8
- Formule: C16H11N3
- Masse moléculaire:245.28
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Paprotrain
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Activité biologique
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MKLP-2 1.35 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| HCT-116 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| HepG2 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| HT-29 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| K562 | GI50 |
21.6 μM
Compound: 1
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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
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[PMID: 26778612] |
| MCF7 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| MDA-MB-231 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| MIA PaCa-2 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
| NCI-H460 | GI50 |
>50 μM
Compound: 1
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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
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[PMID: 26778612] |
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.
Chemical Information
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CAS No. 57046-73-8
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Appearance Solid
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Masse moléculaire 245.28
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Formule C16H11N3
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Color Light yellow to yellow
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SMILES
N#C/C(C1=CNC2=CC=CC=C21)=C\C3=CN=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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J Mol Cell Biol
The mechanoresponsive chromosomal passenger complex sustains furrow ingression under confinement. [Abstract]2025 Jul 22:mjaf019. PMID: 40693957 -
J Cell Sci
An acentrosomal aster with atypical microtubule polarity recruits cytokinesis signals to its center in Xenopus egg extracts. [Abstract]2025 Sep 1:jcs.263766. PMID: 40888042 -
Urol Oncol
Identification of the KIF and MCM protein families as novel targets for combination therapy with CDK4/6 inhibitors in bladder cancer. [Abstract]2023 May;41(5):253.e11-253.e20. PMID: 36813612 -
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Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[2]. Liu J, et al. MKlp2 inhibitor paprotrain affects polar body extrusion during mouse oocyte maturation. Reprod Biol Endocrinol. 2013 Dec 21;11:117. [Content Brief]
[3]. Zhang Y, et al. KIF20A regulates porcine oocyte maturation and early embryo development. [Content Brief]
[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. [Content Brief]
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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