MG PARP Inhibitor VI; NU1025 1PC x 5MG

Biochem/physiol Actions

Cell permeable: no

Reversible: no

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

Product does not compete with ATP.

Primary TargetPARP

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.

Legal Information

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

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.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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.

Warning

Toxicity: Standard Handling (A)