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PJ-34

PARP inhibitor
 
ALX-270-289-M001 1 mg 61.00 USD
 
ALX-270-289-M005 5 mg 150.00 USD
 
ALX-270-289-M025 25 mg 370.00 USD
Do you need bulk/larger quantities?
 
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 Specification

Alternative Name:N-(6-Oxo-5,6-dihydro-phenanthridin-2-yl)-N,N-dimethylacetamide . HCl
 
Formula:C17H17N3O2 . HCl
 
MW:295.2 . 36.5
 
Source:Synthetic.
 
CAS:344458-15-7
 
Purity:≥98% (HPLC)
 
Identity:Determined by 1H-NMR.
 
Appearance:White to light brown or yellow powder.
 
Solubility:Soluble in DMSO (up to 30mg/ml) or water (up to 20mg/ml).
 
Shipping:Ambient
 
Short Term Storage:Ambient
 
Long Term Storage:+4°C
 
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.
 
Handling:Hygroscopic.
 
270-289
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270-289

Product Literature References

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;

Related Products

3-Aminobenzamide 

PARP inhibitor
3544-24-9, ≥97% (GC) | Print as PDF
 
ALX-270-044-G001 1 g 59.00 USD
 
ALX-270-044-G005 5 g 211.00 USD
Do you need bulk/larger quantities?
 

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