Sigma-Aldrich Tdp1 Inhibitor, Cd00509

Assay

≥97% (HPLC)

Quality Level

100

Form

powder

Potency

710 nM IC₅₀

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

yellow

Solubility

DMSO: soluble

Storage Temp.

2-8°C

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.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
Tdp1

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

Dean, R.A., et Al. 2014.J. Biolmol. Screen. 19,1372.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany