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Merck

5.32177

Tdp1 Inhibitor, CD00509

Synonym(s):

Tdp1 Inhibitor, CD00509, Tyrosyl-DNA phosphodiesterase 1 Inhibitor

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About This Item

Empirical Formula (Hill Notation):
C9H6N2O3S
CAS Number:
27430-18-8
Molecular Weight:
222.22
MDL number:
MFCD00020968
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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InChI key

VQRARDATQWRHGF-UHFFFAOYSA-N

InChI

1S/C9H6N2O3S/c12-7-6(4-5-2-1-3-14-5)8(13)11-9(15)10-7/h1-4H,(H2,10,11,12,13,15)

SMILES string

S=C1NC(=O)C(=Cc2[o]ccc2)C(=O)N1

assay

≥97% (HPLC)

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

Quality Level

100

Related Categories

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Tdp1

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

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

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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