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ME 0328

Names

[ CAS No. ]:
1445251-22-8

[ Name ]:
ME 0328

[Synonym ]:
3-(4-oxo-1H-quinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide

Biological Activity

[Description]:

ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC50 of 0.89±0.28 μM.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP
Signaling Pathways >> Epigenetics >> PARP
Research Areas >> Cancer

[Target]

ARTD3/PARP3:0.89 μM (IC50)

ARTD1/PARP1:6.3 μM (IC50)

ARTD2/PARP2:10.8 μM (IC50)

ARTD6/TNKS2:34.3 μM (IC50)

ARTD5/TNKS1:47.3 μM (IC50)

ARTD10/PARP10:71.3 μM (IC50)


[In Vitro]

ME0328 is a potent and selective inhibitor of ARTD3/PARP3 that is active in cells. In in vitro histone H1 modification assay, ME0328 inhibits the transferase activity of ARTD3 with an IC50 of 0.89±0.28 μM. In human A549 cells, ME0328 and ME0355 (at 10 μM) delay the resolution of γH2AX-containing foci that serve as markers for DNA double strand break repair following γ-irradiation (2 Gy). In silico and in vitro physicochemical and metabolic profiling indicated that ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes[1].

[References]

[1]. Lindgren AE, et al. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chem Biol. 2013 Aug 16;8(8):1698-703.


[Related Small Molecules]

Talazoparib | XAV-939 | MK-4827(Niraparib) | Veliparib (ABT-888) | Rucaparib (AG-014699) phosphate | PJ34 HCl | Pamiparib | Rucaparib camsylate | E-7449 | AZD2461 | G007-LK | Iniparib (BSI-201) | NMS-P118 | A-966492 | AG14361

Chemical & Physical Properties

[ Molecular Formula ]:
C19H19N3O2

[ Molecular Weight ]:
321.37300

[ Exact Mass ]:
321.14800

[ PSA ]:
78.60000

[ LogP ]:
3.98570

[ Appearance of Characters ]:
white to beige

[ Storage condition ]:
room temp

[ Water Solubility ]:
DMSO: soluble10mg/mL, clear

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-43

[ Safety Phrases ]:
36/37

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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