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K858

Chemical Structure : K858

CAS No.: 72926-24-0

K858 (K-858, K 858)

Catalog No.: PC-45767Not For Human Use, Lab Use Only.

K858 is a potent, selective inhibitor of mitotic kinesin Eg5 ATPase activity with IC50 of 1.3 uM.

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Biological Activity

K858 is a potent, selective inhibitor of mitotic kinesin Eg5 ATPase activity with IC50 of 1.3 uM.
K858 displays >150-fold more selective for Eg5 than other members of the kinesin superfamily.
K858 induces mitotic arrest, apoptosis, and cell growth inhibition through the activation of the Mad2-mediated spindle checkpoint, and has no effect on microtubule polymerization.
K858 exhibits potent antitumor activity in xenograft models of cancer, and induces the accumulation of mitotic cells with monopolar spindles in tumor tissues.

Physicochemical Properties

M.Wt 277.3421
Formula C13H15N3O2S
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

Acetamide, N-(4-acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)-

References

1. Nakai R, et al. Cancer Res. 2009 May 1;69(9):3901-9.

2. De Iuliis F, et al. Invest New Drugs. 2016 Aug;34(4):399-406.

3. De Monte C, et al. Eur J Med Chem. 2015 Nov 13;105:245-62.

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