Potent, water soluble poly(ADP-ribose) polymerase (PARP) inhibitor (EC50=20nM compared to EC50=200µM of the prototypical PARP inhibitor 3-aminobenzamide (Prod. No. ALX-270-044)). Inhibits peroxynitrite (Prod. No. ALX-400-036)-induced cell necrosis (EC50=20nM). Has significant, dose-dependent, anti-inflammatory effects in a variety of local inflammation models and provides cardioprotection by decreasing myocardial infarct size.
Product Details
| Alternative Name: | N-(6-Oxo-5,6-dihydro-phenanthridin-2-yl)-N,N-dimethylacetamide . HCl |
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| Formula: | C17H17N3O2 . HCl |
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| MW: | 295.2 . 36.5 |
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| Source: | Synthetic. |
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| CAS: | 344458-15-7 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by 1H-NMR. |
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| Appearance: | White to light brown or yellow powder. |
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| Solubility: | Soluble in DMSO (up to 30mg/ml) or water (up to 20mg/ml). |
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| Shipping: | Ambient Temperature |
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| Short Term Storage: | Ambient |
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| Long Term Storage: | +4°C |
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| Use/Stability: | Stable for 2 years after receipt when stored at +4C° (desiccated). Stock solutions are stable for 3 weeks when stored at room temperature. |
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| Handling: | Hygroscopic. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Analysis of PARP inhibitor toxicity by multidimensional fluorescence microscopy reveals mechanisms of sensitivity and resistance: J. Michelena, et al.; Nat. Commun.
9, 2678 (2018),
Abstract;
Full Text
Disrupted ADP-ribose metabolism with nuclear Poly (ADP-ribose) accumulation leads to different cell death pathways in presence of hydrogen peroxide in procyclic Trypanosoma brucei: M. Schlesinger, et al.; Parasit. Vectors
9, 173 (2016),
Application(s): Potency of inhibitors,
Abstract;
Full Text
Microparticle-Induced Activation of the Vascular Endothelium Requires Caveolin-1/Caveolae: A.M. Andrews, et al.; PLoS One.
11, e0149272 (2016),
Application(s): Endothelial cell culture,
Abstract;
Full Text
Regulation of bone morphogenetic protein signaling by ADP-ribosylation: Y. Watanabe, et al.; J. Biol. Chem.
291, 12706 (2016),
Application(s): Cell culture,
Abstract;
Full Text
Effect of poly(ADP-ribose)polymerase and DNA topoisomerase I inhibitors on the p53/p63-dependent survival of carcinoma cells: D. Montariello, et al.; Biochem. Pharmacol.
94, 212 (2015),
Application(s): Cell Culture,
Abstract;
Cytosolic Ca2+ shifts as early markers of cytotoxicity: P. Wyrsch, et al.; Cell Commun. Signal.
11, 11 (2013),
Abstract;
Full Text
Zinc pyrithione impairs zinc homeostasis and upregulates stress response gene expression in reconstructed human epidermis: S.D. Lamore, et al.; Biometals
24, 875 (2011),
Abstract;
PARP1 ADP-ribosylates lysine residues of the core histone tails: S. Messner, et al.; Nucleic Acids Res.
38, 6350 (2010),
Abstract;
Full Text
Pharmacological enhancement of autophagy induced in a hepatocellular carcinoma cell line by high-LET radiation: A. Altmeyer, et al.; Anticancer Res.
30, 303 (2010),
Abstract;
Renal hypoperfusion and impaired endothelium-dependent vasodilation in an animal model of VILI: the role of the peroxynitrite-PARP pathway: R. Vaschetto, et al.; Crit. Care
14, R45 (2010),
Abstract;
The role of PARP activation in glutamate-induced necroptosis in HT-22 cells: X. Xu, et al.; Brain Res.
1343, 206 (2010),
Abstract;
Poly(ADP-ribosyl)ation directs recruitment and activation of an ATP-dependent chromatin remodeler: A.J. Gottschalk, et al.; PNAS USA
106, 13770 (2009),
Abstract;
Substrate-assisted catalysis by PARP10 limits its activity to mono-ADP-ribosylation: H. Kleine, et al.; Mol. Cell
32, 57 (2008),
Abstract;
Systemic and hepatosplanchnic hemodynamic and metabolic effects of the PARP inhibitor PJ34 during hyperdynamic porcine endotoxemia: Z. Ivanyi, et al.; Shock
19, 415 (2003),
Abstract;
Full Text
Activation of poly(ADP-ribose) polymerase contributes to the endothelial dysfunction associated with hypertension and aging: P. Pacher, et al.; Int. J. Mol. Med.
9, 659 (2002),
Abstract;
Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor: R. Faro, et al.; Ann. Thorac. Surg.
73, 575 (2002),
Abstract;
Novel phenanthridinone inhibitors of poly (adenosine 5'-diphosphate-ribose) synthetase: potent cytoprotective and antishock agents: P. Jagtap, et al.; Crit. Care Med.
30, 1071 (2002),
Abstract;
Pharmacologic inhibition of poly(adenosine diphosphate-ribose) polymerase may represent a novel therapeutic approach in chronic heart failure: P. Pacher, et al.; J. Am. Coll. Cardiol.
40, 1006 (2002),
Abstract;
Anti-inflammatory effects of a novel, potent inhibitor of poly (ADP-ribose) polymerase: J.G. Mabley, et al.; Inflamm. Res.
50, 561 (2001),
Abstract;
Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation: F. Garcia Soriano, et al.; Nat. Med.
7, 108 (2001),
Abstract;
Partial protection by poly(ADP-ribose) polymerase inhibitors from nitroxyl-induced cytotoxity in thymocytes: P. Bai, et al.; Free Radic. Biol. Med.
31, 1616 (2001),
Abstract;
Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke: G.E. Abdelkarim, et al.; Int. J. Mol. Med.
7, 255 (2001),
Abstract;
General Literature References
The Therapeutic Potential of Poly(ADP-Ribose) Polymerase Inhibitors: L. Virag and C. Szabo; Pharmacol. Rev.
54, 375 (2002), (Review),
Abstract;
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