MilliporeSigma™ Calbiochem™ Topoisomerase IIα Inhibitor, TSC24

Description

• A cell-permeable, TSC (thiosemicarbazone) derivative that acts as a selective and ATP competitive Topoisomerase IIα inhibitor and Fe chelator
• Independent of its Fe chelating ability, this compound is shown to block Topo II&alpha-catalyzed ATP hydrolysis by competing with ATP for binding to the ATPase domain of Topo IIα (K d = 18μM)
• It also displays M phase cell-cycle arrest at 1μM in nocodazole-treated HT-29 cells
• This compound demonstrates anti-proliferative activity, without distinct or obvious selectivity, towards HeLa, HL-60, SGC7901, and HT-29 cultures (IC 50 = 90 nM, 50 nM, 30 nM, and 20 nM, respectively), and a broader panel of tumor cell lines with IC 50 values in the nanomolar range.