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Description
Overview
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.
Catalogue Number
532177
Brand Family
Calbiochem®
Synonyms
Tyrosyl-DNA phosphodiesterase 1 Inhibitor
References
References
Dean, R.A., et al. 2014. J. Biolmol. Screen.19, 1372.
Dean, R.A., et al. 2014. J. Biolmol. Screen.19, 1372.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
05-January-2015 JSW
Synonyms
Tyrosyl-DNA phosphodiesterase 1 Inhibitor
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.
Form
Yellow powder
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₉H₆N₂O₃S
Purity
≥97% by HPLC
Solubility
DMSO
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Dean, R.A., et al. 2014. J. Biolmol. Screen.19, 1372.