Topoisomerase IIα Inhibitor, TSC24-Calbiochem

C₁₃H₁₄N₄S

258.34

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 = 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.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Huang, H., et al. 2010. J. Med. Chem.53, 3048.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

powder

Calbiochem^®

OK to freeze

yellow

DMSO: 15 mg/mL

wet ice

−20℃

10 mg in Glass bottle

11 - Combustible Solids

WGK 3