PARP inhibitor
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.
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Product Details
Alternative Name |
N-(6-Oxo-5,6-dihydro-phenanthridin-2-yl)-N,N-dimethylacetamide . HCl |
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Appearance |
White to light brown or yellow powder. |
CAS |
344458-15-7 |
Couple Target |
PARP |
Couple Type |
Inhibitor |
Formula |
C17H17N3O2 . HCl |
Identity |
Determined by 1H-NMR. |
MW |
295.2 . 36.5 |
Purity |
≥98% (HPLC) |
Solubility |
Soluble in DMSO (up to 30mg/ml) or water (up to 20mg/ml). |
Source |
Synthetic. |
Handling & Storage
Use/Stability |
As indicated on product label or CoA when stored as recommended. 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. |
Short Term Storage |
Ambient |
Long Term Storage |
+4°C |
Shipping |
Ambient Temperature |
Regulatory Status |
RUO – Research Use Only |
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- The Ubiquitin Ligase TRIP12 Limits PARP1 Trapping and Constrains PARP Inhibitor Efficiency: Gatti, M., Imhof, R., et al.; Cell Rep. 32, 107985 (2020), Abstract
- Poly(ADP-ribose) polymerase 1 accelerates vascular calcification by upregulating Runx2: Wang, C., Xu, W., et al.; Nat. Commun. 10, 1203 (2019), Abstract
- MacroH2A1 Regulation of Poly(ADP-Ribose) Synthesis and Stability Prevents Necrosis and Promotes DNA Repair: Ruiz, P. D., Hamilton, G. A., et al.; Mol. Cell. Biol. 40, (2019), Abstract
- 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
- Necrosis triggered byi>Mycobacterium tuberculosis/i>alters macrophage triglyceride metabolism and inflammatory response in a DGAT1 – dependent manner: Jaisinghani, N., Dawa, S., et al.; bioRxiv , (2017)
- Melatonin regulates PARP1 to control the senescence-associated secretory phenotype (SASP) in human fetal lung fibroblast cells: Yu, S., Wang, X., et al.; J. Pineal Res. 63, (2017), Abstract
- 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
- 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
- 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
- PARP-1 activity is required for the reconsolidation and extinction of contextual fear memory: Inaba, H., Tsukagoshi, A., et al.; Mol. Brain 8, 63 (2015), Abstract
- PARP targeting counteracts gliomagenesis through induction of mitotic catastrophe and aggravation of deficiency in homologous recombination in PTEN-mutant glioma: Majuelos-Melguizo, J., Rodríguez, M. I., et al.; Oncotarget 6, 4790 (2015), Abstract
- MacroH2A1.1 and PARP-1 cooperate to regulate transcription by promoting CBP-mediated H2B acetylation: Chen, H., Ruiz, P. D., et al.; Nat. Struct. Mol. Biol. 21, 981 (2014), 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
- Poly(ADP-ribose)glycohydrolase is an upstream regulator of Ca2+ fluxes in oxidative cell death: Blenn, C., Wyrsch, P., et al.; Cell. Mol. Life Sci. 68, 1455 (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
- The role of PARP activation in glutamate-induced necroptosis in HT-22 cells: X. Xu, et al.; Brain Res. 1343, 206 (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
- 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
- The topical antimicrobial zinc pyrithione is a heat shock response inducer that causes DNA damage and PARP-dependent energy crisis in human skin cells: Lamore, S. D., Cabello, C. M., et al.; Cell Stress Chaperones 15, 309 (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
- Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor: R. Faro, et al.; Ann. Thorac. Surg. 73, 575 (2002), Abstract
- 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
- 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
- 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
- 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
- Anti-inflammatory effects of a novel, potent inhibitor of poly (ADP-ribose) polymerase: J.G. Mabley, et al.; Inflamm. Res. 50, 561 (2001), Abstract
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Alternative Name | 3-AB |
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CAS | 3544-24-9 |
Couple Type | Inhibitor |
Purity | ≥97% (GC) |
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