Biochem/physiol Actions

Primary TargetTdp1

Cell permeable: yes

General description

A cell permeable alkylidene barbiturate analog that acts as a potent and specific inhibitor of tyrosyl-DNA phosphodiesterase 1 (Tdp1; IC₅₀ = 710 nM) and increases the number of g-H2AX foci in MCF-7 cells. Shown to sensitize MCF-7 cells to camptothecin (CPT), increase DNA breaks, and reduce cell proliferation. However, it does not affect the viability of normal mammary epithelial cells up to 10 µM levels. Synergistically reduces cell proliferation and induces apoptosis in MCF-7 cells when combined with Rucaparib, a PARP-1 inhibitor.

Legal Information

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

Other Notes

Dean, R.A., et al. 2014. J. Biolmol. Screen.19, 1372.

Packaging

25 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)