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Beschreibung

A cell-permeable isoquinolinedione compound that potently inhibits PARP-1 activity (pIC50 = 7.35, IC50 = 45 nM) in a NAD+-competitive and reversible manner, while affecting PPAR-2 activity with a 100-fold lower potency. Selectively inhibits PARP-1-mediated cellular PAR formation and is of little effect against PAR formation in fibroblasts derived from parp-1(-/-) mice. Its in vivo application is limited by a poor aqueous solubility (~9 µ,M).