Home Cytoskeletal Signaling Kinesin inhibitor K 858

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K 858 Kinesin inhibitor

Cat.No.S5933

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 Kinesin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 277.34

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (198.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 277.34 Formula

C13H15N3O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 72926-24-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(=O)NC1=NN(C(S1)(C)C2=CC=CC=C2)C(=O)C

Mechanism of Action

Targets/IC50/Ki
Eg5
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.
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.
References

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