528150

PARP Inhibitor VIII, PJ34

The PARP Inhibitor VIII, PJ34, also referenced under CAS 344458-15-7, controls the biological activity of PARP. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): PARP Inhibitor VIII, PJ34
• Empirical Formula (Hill Notation): C₁₇H₁₇N₃O₂ · xHCl
• CAS Number: 344458-15-7
• Molecular Weight: 295.34 (free base basis)
• NACRES: NA.77

Properties

• Quality Level: 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
• shipped in: ambient
• storage temp.: −20°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

Description

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).

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.

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable