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K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $39 | In Stock | In Stock | |
| 10 mg | $64 | In Stock | In Stock | |
| 25 mg | $129 | In Stock | In Stock | |
| 50 mg | $213 | In Stock | In Stock | |
| 100 mg | $326 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | In Stock | 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] |
| Synonyms | 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 27.7 mg/mL (99.88 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.21 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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