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.