493800

PARP Inhibitor VI, NU1025

The PARP Inhibitor VI, NU1025, also referenced under CAS 90417-38-2, controls the biological activity of PARP. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): PARP Inhibitor VI, NU1025, 8-Hydroxy-2-methylquinazoline-4-one
• Empirical Formula (Hill Notation): C₉H₈N₂O₂
• CAS Number: 90417-38-2
• Molecular Weight: 176.17
• MDL number: MFCD00942555
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C9H8N2O2/c1-5-10-8-6(9(13)11-5)3-2-4-7(8)12/h2-4,12H,1H3,(H,10,11,13)
• InChI key: YJDAOHJWLUNFLX-UHFFFAOYSA-N

Description

General description

A potent inhibitor poly(ADP-ribose) polymerase (PARP; IC₅₀ = 0.40 µM). Has been shown to potentiate the cytotoxicity of the DNA-methylating agent MTIC [5-(3-N-methyltriazen-1-yl)-imidazole-4-carboxamide] and ionizing irradiation in murine L210 leukemia cells.

A potent poly(ADP-ribose) polymerase (PARP) inhibitor (IC₅₀ = 400 nM) that potentiates the cytotoxicity of various DNA-active agents, including the DNA-methylating compound MTIC [5-(3-N-methyltriazen-1-yl)-imidazole-4-carboxamide], the DNA strand break-inducing drug temozolomide, topotecan, bleomycin, and ionizing radiation in murine L1210 leukemia cells, Chinese hamster ovary cells, and in a variety of human tumor cell lines.

Biochem/physiol Actions

Cell permeable: no

Primary Target
PARP

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 0.4 µM against poly(ADP-ribose) polymerase (PARP)

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Preparation Note

This solution can be further diluted 1:100 in tissue culture medium before use.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Delaney, C.A., et al. 2000. Clin. Cancer Res.6, 2860.
Boulton, S., et al. 1999. Carcinogenesis20, 199.
Bowman, K.J., et al. 1998. Br. J. Cancer 78, 1269.
Griffin, R.J., et al. 1998. J. Med. Chem. 41, 5247.
Griffin, R.J., et al. 1996. Pharm. Sci. 2, 43.
Boulton, S., et al. 1995. Br. J. Cancer 72, 849.
Griffin, R.J., et al. 1995. Anticancer Drug Res. 10, 507.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3