[CAS NO. 57046-73-8] Paprotrain
PRODUCTS SPECIFICATIONS [57046-73-8]
DESCRIPTION [57046-73-8]
Overview
| MDL | MFCD00617529 |
|---|---|
| Molecular Weight | 245.28 |
| Molecular Formula | C16H11N3 |
| SMILES | N#C/C(C1=CNC2=CC=CC=C21)=C\C3=CN=CC=C3 |
Summary
Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2 , inhibits the ATPase activity of MKLP-2 with an IC 50 of 1.35 μM and a K i of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC 50 of 5.5 μM.
IC50 & Target
|
MKLP-2 1.35 μM (IC 50 ) |
In Vitro
Paprotrain has been screened on a panel of CNS kinases. While inactive (IC 50 >10 μM) on CDK5 and GSK3, it has shown a moderate activity on DYRK1A (IC 50 =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.
Appearance
Solid
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
DMSO : ≥ 100 mg/mL ( 407.70 mM )
* "≥" means soluble, but saturation unknown.
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 |
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1.
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.
- [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.