General description
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 ).
Biochem/physiol Actions
Cell permeable: yes
EC50 = 20 nM inhibiting poly(ADP-ribose) polymerase (PARP)
Primary Target
PARP
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic),protect from light |
| color | white |
| solubility | water: 5 mg/mL |
| web metadata keyword.default | 20 mM PARP Inhibitor VIII PJ34 solution,PARP Inhibitor VIII PJ34 CAS 344458-15-7,PARP Inhibitor VIII PJ34 EC50 = 20 nM,PARP Inhibitor VIII PJ34,PARP inhibitor for cell studies,PARP inhibitor for in vivo models,Sigma-Aldrich PARP Inhibitor VIII PJ34,cell-permeable PARP Inhibitor PJ34,high potency PARP inhibitor PJ34,neuroprotection PARP inhibitor PJ34,phenanthridinone PARP inhibitor for stroke research,research grade PARP Inhibitor VIII PJ34,water-soluble PARP Inhibitor VIII PJ34 |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | Cl.[nH]1c2c(c3c([c]1=O)cccc3)cc(cc2)NC(=O)CN(C)C |
| InChI | 1S/C17H17N3O2.ClH/c1-20(2)10-16(21)18-11-7-8-15-14(9-11)12-5-3-4-6-13(12)17(22)19-15;/h3-9H,10H2,1-2H3,(H,18,21)(H,19,22);1H |
| InChI key | RURAZZMDMNRXMI-UHFFFAOYSA-N |
