ME0328

ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC₅₀ of 0.89±0.28 μM. IC50 & Target: IC50: 0.89±0.28 μM (ARTD3/PARP3), 6.3±0.6 μM (ARTD1/PARP1), 10.8±4.0 μM (ARTD2/PARP2), 34.3±17.0 μM (ARTD6/TNKS2), 47.3±29.0 μM (ARTD5/TNKS1), 71.3±22.0 μM (ARTD10/PARP10)^[1] 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].