614852

Topoisomerase IIα Inhibitor, TSC24

The Topoisomerase IIα Inhibitor, TSC24 controls the biological activity of Topoisomerase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): Topoisomerase IIα Inhibitor, TSC24, (E)-N,N-dimethyl-2-(quinolin-2-ylmethylene)hydrazinecarbothioamide
• Empirical Formula (Hill Notation): C₁₃H₁₄N₄S
• Molecular Weight: 258.34
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• 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

Description

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 (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.

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable