K858 | Kinesin Eg5 inhibitor
NMR (Conforms)
Available Options
| size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $240.00 |
K858 (72926-24-0) is a selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner.1,2 It is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K-858 blocks centrosome separation, activates the spindle checkpoint and induces mitotic arrest accompanied by the formation of monopolar spindles. Displays no effect on microtubule polymerization. Selectively displays antiproliferative effects via induction of mitotic cell death in cancer cells over nontransformed cells.1
References/Citations:
1) Nakai et al. (2009), K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells; Cancer Res., 69 3901
2) Indorato et al. (2013), STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity; Biochem. Pharmacol., 86 1441
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
K858 (72926-24-0) is a selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner.1,2 It is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K-858 blocks centrosome separation, activates the spindle checkpoint and induces mitotic arrest accompanied by the formation of monopolar spindles. Displays no effect on microtubule polymerization. Selectively displays antiproliferative effects via induction of mitotic cell death in cancer cells over nontransformed cells.1
References/Citations:
1) Nakai et al. (2009), K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells; Cancer Res., 69 3901
2) Indorato et al. (2013), STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity; Biochem. Pharmacol., 86 1441
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