PARP Inhibitor VIII, PJ34

A cell-permeable, water-soluble phenanthridinone-derivative that acts as a potent inhibitor of poly(ADP-ribose) polymerase (PARP; EC₅₀ = 20 nM). Shown to be about 10,000 times more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350; EC₅₀ = 200 µM). Does not act as an antioxidant at higher concentrations (1 µM to 10 mM). Exhibits neuroprotection in in vivo and in vitro models of stroke. Also available as a 20 mM solution in H₂O(Cat. No. 528151).

A water-soluble phenanthridinone-derivative that acts as a potent anti-inflammatory agent and an inhibitor of poly(ADP-ribose) polymerase (PARP; EC₅₀ = 20 nM). Shown to be about 10,000-fold more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350) (EC₅₀ = 200 µM). Suppresses neutrophil infiltration and nitric oxide production in peritonitis. Does not act as an antioxidant even at higher concentrations (1 µM to 10 µM). PJ34 inhibits peroxynitrite-induced cell necrosis with an (EC₅₀ = 20 nM). Exhibits neuroprotective effects in in vivo and in vitro models of stroke.

Cell permeable: yes

EC50 = 20 nM inhibiting poly(ADP-ribose) polymerase (PARP)

Primary Target
PARP

Product does not compete with ATP.

Reversible: no

Packaged under inert gas

Toxicity: Standard Handling (A)

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

Abdelkarim, G.E., et al. 2001. Int. J. Mol. Med.7, 255.
Garcia-Soriano, F.G., et al. 2001. Nature Med. 7, 108.
Mabley, G.J., et al. 2001. Inflamm. Res.50, 561.

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