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K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $129 | In Stock | |
50 mg | $213 | In Stock | |
100 mg | $326 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
Description | K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner. |
Targets&IC50 | EG5:1.3 μM |
In vitro | K858 is an ATP-uncompetitive inhibitor of Eg5 that is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K858 induces mitotic arrest and growth inhibition through the activation of the Mad2-mediated spindle checkpoint. K858 induces mitotic cell death in Y cells but not in normal cells. K858 induces mitotic arrest, apoptosis, and cell growth inhibition and has no effect on microtubule polymerization. |
In vivo | K858 exhibits antitumor activity and induces mitotic arrest in a human tumor xenograft mouse model. K858 exhibits antitumor activity and induces mitotic arrest in human xenograft tumor models. [1] |
Alias | K858 Racemic, K858 |
Molecular Weight | 277.34 |
Formula | C13H15N3O2S |
Cas No. | 72926-24-0 |
Smiles | CC(=O)NC1=NN(C(C)=O)C(C)(S1)c1ccccc1 |
Relative Density. | 1.27 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 27.7 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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