[CAS NO. 72926-24-0] K 858
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PRODUCTS SPECIFICATIONS [72926-24-0]
Store
Catalog
SLK-S5933
Brand
Selleck
CAS
72926-24-0
DESCRIPTION [72926-24-0]
Overview
| MDL | MFCD00181155 |
|---|---|
| Molecular Weight | 277.34 |
| Molecular Formula | C13H15N3O2S |
| SMILES | CC(NC1=NN(C(C)=O)C(C2=CC=CC=C2)(C)S1)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6057 mL | 18.0284 mL | 36.0568 mL |
| 5 mM | 0.7211 mL | 3.6057 mL | 7.2114 mL |
| 10 mM | 0.3606 mL | 1.8028 mL | 3.6057 mL |
| 50 mM | 0.0721 mL | 0.3606 mL | 0.7211 mL |
Description
K858 is a novel and potent inhibitor of 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.
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.
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