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Medchemexpress LLC K858 (Racemic) | 72926-24-0 | 99.8% | 277.34 | 25 MG

Supplier: Medchemexpress LLC 25MGHY19966
K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.
- Does not inhibit the ATPase activity of the mitotic kinesins CENP-E and MKLP1, or the conventional kinesin heavy chain even at 200 μM.
- Induces mitotic arrest and growth inhibition via the activation of the Mad2-mediated spindle checkpoint.
- Induces mitotic cell death in cancer cells but not in normal cells (at 5 μM).
- Shows antitumor activity in an A2780 ovarian cancer xenograft model, and also inhibits tumor growth in a HCT116 colon cancer xenograft model.
- Displays no neurotoxic side effects in mice (at 100 mg/kg, p.o., qd x5).
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