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PARP Inhibitor IX, EB-47

Names

[ CAS No. ]:
366454-36-6

[ Name ]:
PARP Inhibitor IX, EB-47

[Synonym ]:
4-[1-(6-Amino-9H-purin-9-yl)-1-deoxy-|A-D-ribofuranuronoyl]-N-(2,3-dihydro-1-oxo-1H-isoindol-4-yl)-1-piperazineacetamide Dihydrochloride
5'-Deoxy-5'-[4-[2-[(2,3-dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5'-oxoadenosine Dihydrochloride
EB 47

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PARP
Research Areas >> Cardiovascular Disease
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

ARTD1/PARP1:45 nM (IC50)


[In Vitro]

EB-47 shows inhibition in excess of 50% with CdPARP, and it is able to inhibit CdPARP and HsPARP with IC50 values of 0.86 and 1.0 µM, respectively[1].

[In Vivo]

EB-47 (2 μM; 5 days) decreases the number of embryo implantation sites and blastocysts at day 5. PARP1 participates in the process of embryo implantation[3].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H27N9O6

[ Molecular Weight ]:
537.52800

[ Exact Mass ]:
537.20800

[ PSA ]:
208.04000

Related Compounds