ME-0328

• CAT Number: R060638
• CAS Number: 1445251-22-8
• Molecular Formula: C₁₉H₁₉N₃O₂
• Molecular Weight: 321.37
• Purity: ≥95%
• Target: PARP
• Solubility: Soluble in DMSO > 10 mM
• Storage: Store at -20 C
• InChI: InChI=1S/C19H19N3O2/c1-13(14-7-3-2-4-8-14)20-18(23)12-11-17-21-16-10-6-5-9-15(16)19(24)22-17/h2-10,13H,11-12H2,1H3,(H,20,23)(H,21,22,24)/t13-/m0/s1
• InChIKey: QIHBWVVVRYYYRO-ZDUSSCGKSA-N
• SMILES: CC(C1=CC=CC=C1)NC(=O)CCC2=NC(=O)C3=CC=CC=C3N2

ME0328 is an inhibitor of PARP-3 (IC50 = 0.89 μM). ME0328 displays selectivity for PARP-3 over PARP-1, PARP-2 and other ARDT enzymes (IC50 values are 6.3, 10.8 and >30 μM respectively). ME0328 also enhances CRISPR-Cas9-mediated HER2 mutation frequency, resulting in increased reduction in proliferation of HER2-positive breast cancer cells.

Reference

1: Lindgren AE, Karlberg T, Thorsell AG, Hesse M, Spjut S, Ekblad T, Andersson CD, Pinto AF, Weigelt J, Hottiger MO, Linusson A, Elofsson M, Schüler H. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chem Biol. 2013 Aug 16;8(8):1698-703. doi: 10.1021/cb4002014. PubMed PMID: 23742272.