A PARP1 inhibitor
Poly(ADP-ribose) polymerase 1 (PARP1) is a critical DNA repair enzyme involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions including ischemia and reperfusion injury, asthma-related inflammation, and atherogenesis. TIQ-A is a PARP1 inhibitor (IC50 = 450 nM in cultured mouse cortical neurons). It displays neuroprotective effects in cultured mouse cortical neurons injured by oxygen-glucose deprivation (IC50 = 0.15 µM). TIQ-A has been used to inhibit eosinophilic infiltration into airways of OVA-challenged mice and to induce the regression of atherosclerotic plaques in high-fat fed apolipoprotein E(-/-) mice.
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