An inhibitor of Eg5 (IC50 = 1.3 µM); inhibits growth (GI50 = 0.98 µM)

K858 – 5 mg

Brand:
Cayman
CAS:
72926-24-0
Storage:
-20
UN-No:
Non-Hazardous - /

K858 is an inhibitor of kinesin spindle protein Eg5 (IC50 = 1.3 µM for Eg5 ATPase activity).{46342} 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.  

 

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Description

An inhibitor of Eg5 (IC50 = 1.3 µM); inhibits growth (GI50 = 0.98 µM), induces mitotic arrest (EC50 = 1.6 µM), and activates caspase-3 (EC50 = 1.6 µM) in HCT116 cells; selectively induces mitotic cell death in HCT116 cells over non-cancerous ARPE-19 retinal pigment epithelial cells; reduces tumor growth in an A2780 ovarian cancer mouse xenograft model at 150 mg/kg

Formal name: N-(4-acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)-acetamide

Synonyms: 

Molecular weight: 277.3

CAS: 72926-24-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis

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