Chemical Structure : K858
CAS No.: 72926-24-0
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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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.
M.Wt | 277.3421 | |
Formula | C13H15N3O2S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Acetamide, N-(4-acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)- |
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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