1190332-25-2

1190332-25-2 structure

Name: EB 47, PARP-1 inhibitor
Chemical Name: 2-(4-{[(2R,3R,4S,5S)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxytetrahydro-2-furanyl]carbonyl}-1-piperazinyl)-N-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)acetamide dihydrochloride
CAS Number: 1190332-25-2
Molecular Formula: C₂₄H₂₉Cl₂N₉O₆
Molecular Weight: 610.450
Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
Create Date: 2018-07-17 09:01:28
Modify Date: 2024-01-06 13:40:57
EB-47 dihydrochloride, 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].

Name	2-(4-{[(2R,3R,4S,5S)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxytetrahydro-2-furanyl]carbonyl}-1-piperazinyl)-N-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)acetamide dihydrochloride
Synonyms	2-(4-{[(2R,3R,4S,5S)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxytetrahydro-2-furanyl]carbonyl}-1-piperazinyl)-N-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)acetamide dihydrochloride

Description	EB-47 dihydrochloride, 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 >> Inflammation/Immunology Signaling Pathways >> Cell Cycle/DNA Damage >> PARP
In Vitro	EB-47 dihydrochloride 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 dihydrochloride (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]. 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.