| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Paprotrain targets MKLP-2 (KIF20A), a kinesin-6 family member involved in cytokinesis and mitotic progression. MKLP-2 is essential for the central spindle formation and completion of cytokinesis during cell division. By inhibiting MKLP-2 ATPase activity, paprotrain disrupts mitotic progression and cytokinesis, leading to cell cycle arrest and potential cell death. The compound is also known as a passenger proteins transport inhibitor.
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| ln Vitro |
Paprotrain has been tested against a panel of CNS kinases. While inert against CDK5 and GSK3 (IC50 >10 μM), it has moderate action against DYRK1A (IC50=5.5 μM) [1]. Time-lapse microscopy revealed that pabroterin disrupted MKlp2 expression, resulting in polar body extrusion failure. This can be recovered by removing oocytes from pabrolin in fresh culture medium. According to cell cycle analysis, the majority of oocytes were arrested in metaphase I or telophase I. However, even after paprotrain suppresses MKlp2, the oocyte spindle structure and chromosomal organization remain intact [2]. The nuclear maturation of porcine oocytes treated with Paprotrain failed. After inhibiting KIF20A activity, the number of oocytes halted in the early MI stage rose in a dose-dependent manner, while the percentage of oocytes reaching the ATI and MII stages dropped [3].
In vitro, paprotrain inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 microM and a Ki of 3.36 microM. It inhibits both basal and microtubule/MT-stimulated ATPase activity with IC50 values of 1.35 and 0.83 microM, respectively. The compound's cell-permeable nature allows it to enter cells and inhibit MKLP-2 function in cellular assays. Its activity has been characterized in biochemical assays measuring ATP hydrolysis and in cell-based assays assessing mitotic progression. |
| ln Vivo |
In vivo activity of paprotrain is inferred from its mechanism as an MKLP-2 inhibitor. By disrupting cytokinesis, the compound may have antitumor effects in cancer cells that are dependent on proper mitotic progression. However, detailed in vivo data for paprotrain are limited in the available literature. The compound is a research tool for studying the role of MKLP-2 in cell division and cancer.
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| Enzyme Assay |
The in vitro enzyme assay for paprotrain involves measuring MKLP-2 ATPase activity. Purified MKLP-2 protein is incubated with varying concentrations of paprotrain (typically 0.001-100 uM) in the presence of ATP and microtubules in assay buffer at 37degC for 30-60 minutes. The ATPase activity is measured using a coupled enzyme assay where ATP hydrolysis is linked to NADH oxidation, monitored spectrophotometrically at 340 nm. Alternatively, a malachite green phosphate detection assay can be used to quantify inorganic phosphate released from ATP hydrolysis. IC50 values are determined by fitting inhibition data to a dose-response curve.
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| Cell Assay |
In vitro cellular assays for paprotrain are conducted using cancer cell lines to assess its effects on mitosis and cytokinesis. Cells are seeded in multi-well plates and treated with varying concentrations of paprotrain (typically 0.01-100 uM) for 24-72 hours. Cell viability is assessed using MTT, CellTiter-Glo, or crystal violet staining assays. Cell cycle analysis is performed by flow cytometry using propidium iodide staining to assess the accumulation of cells in specific cell cycle phases. Cytokinesis failure is assessed by scoring binucleated cells or by immunofluorescence staining for alpha-tubulin and other mitotic markers. Apoptosis is evaluated using Annexin V-FITC/PI double staining.
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| Animal Protocol |
In vivo animal studies for paprotrain typically involve xenograft models in immunodeficient mice bearing human tumor cell lines. Mice are implanted subcutaneously with cancer cells. When tumors reach a volume of approximately 100-200 mm3, mice are randomized to receive paprotrain or vehicle control. The compound is administered by intraperitoneal injection at doses determined from preliminary pharmacokinetic and tolerability studies. Tumor volumes are measured twice weekly with calipers, and body weights are monitored for toxicity. At study termination, tumors are excised for histological analysis and biomarker evaluation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of paprotrain are not extensively documented. The compound has a molecular weight of 245.28 and a molecular formula of C16H11N3. It appears as a yellow powder or solid. The compound should be stored at -20degC and protected from light. As a small, cell-permeable molecule, it is expected to have good oral bioavailability and the ability to cross cell membranes. Detailed ADME parameters are not available in the published literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of paprotrain has not been extensively characterized. As an MKLP-2 inhibitor that disrupts mitosis and cytokinesis, the compound may have effects on rapidly dividing tissues including bone marrow, gastrointestinal epithelium, and hair follicles. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions should be followed when handling the compound in a laboratory setting. No specific LD50 values have been reported.
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| References | |
| Additional Infomation |
Paprotrain (CAS 57046-73-8) is a cell-permeable inhibitor of MKLP-2 (KIF20A), a kinesin-6 family member involved in cytokinesis. It inhibits MKLP-2 ATPase activity with an IC50 of 1.35 microM and a Ki of 3.36 microM. The compound is a research tool for studying the role of MKLP-2 in cell division and cancer. It is available for research purposes only.
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| Molecular Formula |
C16H11N3
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|---|---|
| Molecular Weight |
245.2786
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| Exact Mass |
245.095
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| CAS # |
57046-73-8
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| PubChem CID |
12248889
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
470.1±40.0 °C at 760 mmHg
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| Flash Point |
149.2±12.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.739
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| LogP |
3.17
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C(=CN2)/C(=C/C3=CN=CC=C3)/C#N
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| InChi Key |
YMYYQRZCCKBFBE-MDWZMJQESA-N
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| InChi Code |
InChI=1S/C16H11N3/c17-9-13(8-12-4-3-7-18-10-12)15-11-19-16-6-2-1-5-14(15)16/h1-8,10-11,19H/b13-8+
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| Chemical Name |
(Z)-2-(1H-indol-3-yl)-3-pyridin-3-ylprop-2-enenitrile
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~407.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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