Home Cytoskeletal Signaling Kinesin inhibitor K 858 For research use only.

K 858

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.

K 858 Chemical Structure

K 858 Chemical Structure

CAS No. 72926-24-0

Purity & Quality Control

Batch: S593301 DMSO]55 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

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Signaling Pathway

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models BALB/cAJcl-nu mice inoculated with A2780 cells
Dosages 150 and 50 mg/kg
Administration oral

Chemical Information & Solubility

Molecular Weight 277.34 Formula

C13H15N3O2S
CAS No. 72926-24-0 SDF --
Smiles CC(=O)NC1=NN(C(S1)(C)C2=CC=CC=C2)C(=O)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 55 mg/mL ( (198.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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