K-858, Kinesin Eg5 inhibitor (TBI1312)

Description

Product Details

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

Molecular Formula: C₁₃H₁₅N₃O₂S

Formula Weight: 277.35

CAS Number: 72926-24-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml)

Storage: RT

Stability: ≥ 1 year.

Applications

Kinesin Eg5 inhibitor

Functions

Selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner. It is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K858 blocks centrosome separation, activates the spindle checkpoint and induces mitotic arrest accompanied by the formation of monopolar spindles. Displays no effect on microtubule polymerization. Selectively displays antiproliferative effects via induction of mitotic cell death in cancer cells over nontransformed cells.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.