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.
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Huang, H., et al. 2010. J. Med. Chem.53, 3048.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 258.34. Empirical Formula: C13H14N4S. Quality Level: 100. Assay: ≥. 95% (HPLC). form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze. color: yellow. solubility: DMSO: 15 . mg/mL. shipped in: wet ice. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51141528
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 614852-10MG