KU-0058948

A PARP1 and PARP2 inhibitor (IC50s = 3.4 and 1.5 nM, respectively), selective for PARP1 over PARP3, PARP4, and tankyrase (IC50s = 40, 1,200, and >10,000 nM, respectively), selectively inhibits the survival of embryonic stem cells lacking Brca1 or Brca2 over embryonic stem cells expressing wild-type Brca1 or Brca2, decreases the survival and induces apoptosis in P39 and MUTZ-3 AML cells at 1 µM, potentiates MS-275-induced cytotoxicity in patient-derived AML cells at 5 nM, reduces survival in PTEN-deficient HCT116 cells but not those expressing wild-type PTEN or HCT116+/neo. Formulation: A solid. InChI: InChI=1S/C21H21FN4O2/c22-18-7-6-14(12-17(18)21(28)26-10-3-8-23-9-11-26)13-19-15-4-1-2-5-16(15)20(27)25-24-19/h1-2,4-7,12,23H,3,8-11,13H2,(H,25,27). InChIKey: HGEPGGJUGUMFHT-UHFFFAOYSA-N. SMILES: FC(C(C(N1CCNCCC1)=O)=C2)=CC=C2CC3=NNC(C4=C3C=CC=C4)=O