EB-47

EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD+?and extends from the nicotinamide to the adenosine subsite[1].

[1]Haikarainen T, et al. Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.ACS Med Chem Lett. 2013 Nov 20;5(1):18-22.|[2]García-Saura AG, et al. Comparative inhibitory profile and distribution of bacterial PARPs, using Clostridioides difficile CD160 PARP as a model. Sci Rep. 2018 May 23;8(1):8056.|[3]Joshi A, et al.PARP1 during embryo implantation and its upregulation by oestradiol in mice.Reproduction. 2014 Jun;147(6):765-80.|[4]Jagtap PG, et al. The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).Bioorg Med Chem Lett. 2004 Jan 5;14(1):81-5.Research Square Preprint. 2022 Feb.|Nucleic Acids Res. 2023 Jun 16;gkad515.|University of New Mexico. 2024 Jul 01.