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Product Details

K858 | Kinesin Eg5 inhibitor

K858 (72926-24-0) is a selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner1,2. 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 cells1.

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., Epub ahead of print Sept. 13

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K-858 | 72926-24-0 | Structure | Supplier

Catalog#  10-1312

$60.00
Quantity
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CAS:
72926-24-0
Catalog Number:
10-1312
Activity:
Kinesin Eg5 inhibitor
Chemical Name:
N-(4-Acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide
Molecular Weight:
277.35
Molecular Formula:
C13H15N3O2S
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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