K 858

Catalog No.S5933

K 858 Chemical Structure

Molecular Weight(MW): 277.34

K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily.

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Biological Activity

Description K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily.
Targets
Eg5 [1]
()
1.3 μM
In vitro

K858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. Long-term continuous treatment of cancer cells with K858 resulted in antiproliferative effects through the induction of mitotic cell death, and polyploidization followed by senescence. In contrast, treatment of nontransformed cells with K858 resulted in mitotic slippage without cell death, and cell cycle arrest in G1 phase in a tetraploid state. K858 has minimal effects on abnormalities in the number and structure of chromosomes. K858 has no effect on microtubule polymerization in cell-free and cell-based assays[1].

In vivo K858 exhibits potent antitumor activity in xenograft models of cancer, and induces the accumulation of mitotic cells with monopolar spindles in tumor tissues. K858 is not neurotoxic in a motor coordination test in mice[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HCT116 cells
  • Concentrations: 3 μM
  • Incubation Time: 18 h
  • Method:

    HCT116 cells are treated with vehicle, paclitaxel, vincristine, K858, or monastrol for 18 h.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: BALB/cAJcl-nu mice inoculated with A2780 cells
  • Formulation: 0.5% methylcellulose 400
  • Dosages: 150 and 50 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 55 mg/mL (198.31 mM)
Ethanol 4 mg/mL (14.42 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 277.34
Formula

C13H15N3O2S

CAS No. 72926-24-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Kinesin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID