1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEME0328Cat. No.: HY-100225CAS No.: 1445251-22-8分式: CHNO分量: 321.37作靶點(diǎn): PARP作通路: Cell Cycle/DNA Damage; Epigenetics儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 75 mg/mL (233.38 mM; Need ult

2、rasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.78 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 ME0328種有效的選擇性 ARTD3/PARP3 抑制劑，IC50 為 0.890.28 M。IC50 & Target ARTD3/PARP3 ARTD1/PARP1 ARTD2/PARP2 ARTD6/TNKS20.89 M (IC50) 6.3 M (IC50

3、) 10.8 M (IC50) 34.3 M (IC50)ARTD5/TNKS1 ARTD10/PARP1047.3 M (IC50) 71.3 M (IC50)體外研究 ME0328 is a potent and selective inhibitor of ARTD3/PARP3 that is active in cells. In in vitro histone H1modification assay, ME0328 inhibits the transferase activity of ARTD3 with an IC50 of 0.890.28 M. In humanA54

4、9 cells, ME0328 and ME0355 (at 10 M) delay the resolution of H2AX-containing foci that serve asmarkers for DNA double strand break repair following -irradiation (2 Gy). In silico and in vitro physicochemicaland metabolic profiling indicated that ME0328 is soluble, cell permeable, and metabolically s

5、table in human livermicrosomes and rat hepatocytes 1.REFERENCES1. Lindgren AE, et al. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chem Biol. 2013 Aug16;8(8):1698-703.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-5895