1445251-22-8 Usage
Description
ME0328 is a potent and selective poly ADP ribose polymerase (PARP) inhibitor, specifically targeting the human ADP-Ribosyltransferase ARTD3/PARP3. It is an enzyme that plays a crucial role in DNA repair, apoptosis, inflammation, and other cellular processes, particularly in response to reactive oxygen and nitrogen species. ME0328 is cell permeable and can elicit PARP3-specific effects at submicromolar concentrations.
Uses
Used in Pharmaceutical Industry:
ME0328 is used as a PARP inhibitor for its role in regulating DNA repair and mitotic progression. Its selectivity for PARP3 over other PARP family members makes it a valuable compound in the development of targeted therapies for various diseases, including cancer.
Used in Cancer Research:
ME0328 is used as a research tool to study the role of PARP3 in cancer cell biology. Its ability to inhibit PARP3 at submicromolar concentrations allows researchers to investigate the specific effects of PARP3 inhibition on cancer cell growth, survival, and response to other treatments.
Used in Drug Development:
ME0328 is used as a lead compound in the development of new drugs targeting PARP3 for the treatment of cancer and other diseases. Its selectivity and potency make it an attractive starting point for the design and optimization of more effective and specific PARP3 inhibitors.
Used in DNA Repair Mechanisms:
ME0328 is used to study the role of PARP3 in DNA repair mechanisms, particularly in the context of its regulation of DNA repair and mitotic progression. Understanding the function of PARP3 in these processes can provide insights into the development of novel therapeutic strategies for diseases associated with DNA repair defects.
Used in Apoptosis and Inflammation Research:
ME0328 is used to investigate the role of PARP3 in apoptosis and inflammation, as these processes are also regulated by PARP enzymes. By inhibiting PARP3, researchers can gain a better understanding of the molecular mechanisms underlying these cellular events and potentially identify new targets for therapeutic intervention.
References
1) Lindgren?et al. (2013),?PARP Inhibitor with Selectivity Toward ADP-Ribosyltransferase ART3/PARP3; ACS Chem. Biol.,8?1689
Check Digit Verification of cas no
The CAS Registry Mumber 1445251-22-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,4,5,2,5 and 1 respectively; the second part has 2 digits, 2 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1445251-22:
(9*1)+(8*4)+(7*4)+(6*5)+(5*2)+(4*5)+(3*1)+(2*2)+(1*2)=138
138 % 10 = 8
So 1445251-22-8 is a valid CAS Registry Number.
1445251-22-8Relevant articles and documents
Chemical probes to study ADP-ribosylation: Synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3
Lindgren, Anders E.G.,Karlberg, Tobias,Ekblad, Torun,Spjut, Sara,Thorsell, Ann-Gerd,Andersson, C. David,Nhan, Ton Tong,Hellsten, Victor,Weigelt, Johan,Linusson, Anna,Schüler, Herwig,Elofsson, Mikael
, p. 9556 - 9568 (2014/01/06)
The racemic 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[1-(pyridin-2-yl)ethyl] propanamide, 1, has previously been identified as a potent but unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3). Herein we describe synthesis and evaluation of 55 compounds in this class. It was found that the stereochemistry is of great importance for both selectivity and potency and that substituents on the phenyl ring resulted in poor solubility. Certain variations at the meso position were tolerated and caused a large shift in the binding pose. Changes to the ethylene linker that connects the quinazolinone to the amide were also investigated but proved detrimental to binding. By combination of synthetic organic chemistry and structure-based design, two selective inhibitors of ARTD3 were discovered.
