5.32177

Tdp1 Inhibitor, CD00509

• Synonym(s): Tdp1 Inhibitor, CD00509, Tyrosyl-DNA phosphodiesterase 1 Inhibitor
• Empirical Formula (Hill Notation): C₉H₆N₂O₃S
• CAS Number: 27430-18-8
• Molecular Weight: 222.22
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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: yes

Primary 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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable