4-HQN (491-36-1) is an inhibitor of poly(ADP-ribose) polymerase (PARP) (IC50 = 9.5 μM).1 Displays mixed inhibition with respect to NAD+. Protective against ischemia-reperfusion induced ROS production, and subsequent mitochondrial and cell damage in rat heart.2 4-HQN is anti-inflammatory in LPS-induced endotoxic mice in vivo; decreases NF-κB and AP-1 activation.3
References/Citations:
1) Banasil et al. (1992), Specific inhibitors of poly(ADP-ribose) synthetase and mono(ADP-ribosyl)transferase; J. Biol. Chem., 267 1569
2) Halmosi et al. (2001), Effect of poly(ADP-ribose) polymerase inhibitors on the ischemia-reperfusion-induced oxidative cell damage and mitochondrial metabolism in Langendorff heart perfusion system. Clin. Mol. Pharmacol., 59 1497
3) Veres et al. (2004), Regulation of kinase cascades and transcription factors by a poly(ADP-ribose) polymerase-1 inhibitor, 4-hydroxyquinazoline, in lipopolysaccharide-induced inflammation in mice; J. Pharmacol. Exp. Ther., 310 247
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