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Paprotrain

Chemical Structure : Paprotrain

CAS No.: 57046-73-8

Paprotrain

Catalog No.: PC-22648Not For Human Use, Lab Use Only.

Paprotrain is a selective, reversible inhibitor of KIF20A (mitotic kinesin-like protein 2, MKLP-2, MKlp2) with Ki of 3.4 uM, does not inhibit other members of the kinesin superfamily.

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Biological Activity

Paprotrain is a selective, reversible inhibitor of KIF20A (mitotic kinesin-like protein 2, MKLP-2, MKlp2) with Ki of 3.4 uM, does not inhibit other members of the kinesin superfamily.
Paprotrain exhibits IC50 values of 1.35 μM in basal and 0.83 μM in MT-stimulated ATPase assays.
Paprotrain is cell permeable and incubation with 10 to 50 μM inhibitor results in binucleated cells, a characteristic phenotype similar to that observed following RNAi-mediated depletion of MKLP-2.
Paprotrain induces mitotic spindle defects, perturbs MKLP-2-mediated relocation of the chromosome passenger proteins Aurora B and survivin from the centromeres to the central spindle.
Paprotrain does not impair kinesin family member 4 (Kif4)-mediated translocation of protein regulating cytokinesis 1 (PRC1), which emphasizes its specificity for MKLP-2.

Physicochemical Properties

M.Wt 245.29
Formula C16H11N3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-2-(1H-Indol-3-yl)-3-(pyridin-3-yl)acrylonitrile

References

1. Tcherniuk S, et al. Angew Chem Int Ed Engl. 2010 Oct 25;49(44):8228-31.

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