PARP Inhibitor IX, EB-47

Modify Date: 2024-01-10 22:46:15

PARP Inhibitor IX, EB-47 structure	Common Name	PARP Inhibitor IX, EB-47
	CAS Number	366454-36-6	Molecular Weight	537.52800
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₄H₂₇N₉O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of PARP Inhibitor IX, 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].

Name	2-[4-[(2R,3R,4S,5S)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolane-2-carbonyl]piperazin-1-yl]-N-(1-oxo-2,3-dihydroisoindol-4-yl)acetamide
Synonym	More Synonyms

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.

Molecular Formula	C₂₄H₂₇N₉O₆
Molecular Weight	537.52800
Exact Mass	537.20800
PSA	208.04000

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

PARP Inhibitor IX, EB-47

Use of PARP Inhibitor IX, EB-47

Names

PARP Inhibitor IX, EB-47 Biological Activity

Chemical & Physical Properties

Synonyms