K858

K858 is an inhibitor of kinesin spindle protein Eg5 (IC50 = 1.3 µM for Eg5 ATPase activity). 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.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: DMF: 25 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 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.