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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C13H14N4S
Molecular Weight:
258.34
NACRES:
NA.54
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze
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Quality Level

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

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.

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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