An inhibitor of Eg5
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K858

Item No. 22112

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)-acetamide
CAS Number
72926-24-0
Molecular Formula
C13H15N3O2S
Formula Weight
277.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
221, 289 nm
SMILES
O=C(C)N1N=C(NC(C)=O)SC1(C)C2=CC=CC=C2
InChi Code
InChI=1S/C13H15N3O2S/c1-9(17)14-12-15-16(10(2)18)13(3,19-12)11-7-5-4-6-8-11/h4-8H,1-3H3,(H,14,15,17)
InChi Key
JEFVYQYZCAVNTP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $77

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    10 mg

    $135

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    25 mg

    $294

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    Cayman Chemical
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    Product Description

    K858 is an inhibitor of kinesin spindle protein Eg5 (IC50 = 1.3 µM for Eg5 ATPase activity).1 It inhibits growth (GI50 = 0.98 µM), induces mitotic arrest (EC50 = 1.6 µM), and activates caspase-3 (EC50 = 1.6 µM) in HCT116 cells. It selectively induces mitotic cell death in HCT116 cells over non-cancerous ARPE-19 retinal pigment epithelial cells. K858-treated HCT116 cells that escape mitotic cell death undergo polyploidization and senescence. K858 reduces tumor growth in an A2780 ovarian cancer mouse xenograft model when administered at a dose of 150 mg/kg and increases the number of mitotic cells with monopolar spindles in tumor tissue.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nakai, R., Iida, S., Takahashi, T., et al. K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells. Cancer Res. 69(9), 3901-3909 (2009).