Non disponible en dehors du Royaume-Uni et de l'Irlande
General 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 (Kd = 18 µM). It also displays M phase cell-cycle arrest at 1 µM 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 (IC50 = 90 nM, 50 nM, 30 nM, and 20 nM, respectively), and a broader panel of tumor cell lines with IC50 values in the nanomolar range.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Huang, H., et al. 2010. J. Med. Chem.53, 3048.
Packaging
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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