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ME0328PARP inhibitor,potent and selective

ME0328

Catalog No. A8808
Size Price Stock Qty
10mM (in 1mL DMSO) $50.00 In stock
10mg $68.00 In stock
50mg $329.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

ME0328

Biological Activity

ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Targets PARP3 PARP1        
IC50 0.89μM 6.3μM        

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Chemical Properties

Cas No. 1445251-22-8 SDF Download SDF
Chemical Name 3-(4-oxo-1H-quinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide
Canonical SMILES CC(C1=CC=CC=C1)NC(=O)CCC2=NC(=O)C3=CC=CC=C3N2
Formula C19H19N3O2 M.Wt 321.37
Solubility Soluble in DMSO > 10 mM Storage Store at -20° C
General tips N/A
Shipping Condition N/A

Background

ME0328 is a potent and selective inhibitor of PARP with IC50 value of 0.89 and 6.3 μM for PARP3 and PARP1, respectively [1].

Poly (ADP-ribose) polymerase (PARP) is a family of proteins mainly involved in programmed cell death and DNA repair. The overactivation of PARP may reduce the stores of cellular NAD+ and induce ATP depletion and cell death.

ME0328 is a potent and selective PARP inhibitor. ME0328 selectively inhibited ADP-ribosyltransferase-3/poly(ADP-ribose) polymerase-3 (ARTD3) with IC50 value of 0.89 μM and inhibited ARTD1 and ARTD2 with IC50 values of 6.3 and 10.8 μM, respectively. In human alveolar basal epithelial (A549) cells, treatment with ME0355 (10 μM) followed by γ-irradiation significantly delayed γH2AX-foci resolution in a concentration-dependent way, which suggested that ME0328 inhibited ARTD3 in cells. In nonirradiated human A549 and mouse MRC5 cells, ME0328 (10 μM) did not exhibit toxicity [1].

Reference:
[1].  Lindgren AE, Karlberg T, Thorsell AG, et al. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chem Biol, 2013, 8(8): 1698-1703.