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Medchemexpress LLC K858 (Racemic) | 72926-24-0 | 99.83% | 277.35 | 10 MM * 1 ML
SDP

Supplier:  Medchemexpress LLC HY1996610MM/1ML

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K858 (Racemic) is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM. It is intended for research use only and is not sold to patients.

  • Acts as an ATP-uncompetitive inhibitor of kinesin Eg5 (IC50 of 1.3 μM).
  • Induces mitotic arrest and growth inhibition by activating the Mad2-mediated spindle checkpoint.
  • Induces mitotic cell death in cancer cells but not in normal cells at 5 μM.
  • Inhibits MCF7, BT474, and SKBR3 cell lines at 10 and 100 μM, and MDA-MB231 cell line at 10 and 100 μM after 24 hours.
  • Increases Bax/Bcl2 RNA ratio and survivin in four cell lines.
  • Upregulation of survivin is reversed by wortmannin (phosphoinositide 3-kinase AKT) in MCF7 cells.
  • Shows antitumor activity in A2780 ovarian cancer xenograft and HCT116 colon cancer xenograft models.
  • No neurotoxic side effects observed in mice at 100 mg/kg.

Catalog No. 50-004-05074


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