For research use only. Not for therapeutic Use.
Potent and specific PARP inhibitor (IC50: 3.4 nM for PARP1); KU-0058948 activates transfected extracellular signal-regulated kinase 8 (ERK8) in cells and induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines in vitro. The freebase, KU-0058948 (Axon 4179) is also available.
KEYWORDS: KU-0058948 hydrochloride | supplier | PARP1 inhibitor | KU-58948 | KU0058948 | KU58948 | KU 0058948 | KU 058948 | CAS [763111-49-5] | [2108829-86-1] | DNA-RNA | PARP | ERK8 | extracellular signal-regulated kinase 8 | cell cycle arrest | apoptosis | repair | Poly(ADP-Ribose) Polymerase
| Catalog Number | I047589 |
| CAS Number | 2108829-86-1 |
| Molecular Formula | C21H21FN4O2.HCl |
| Purity | ≥95% |
| IUPAC Name | 4-[[3-(1,4-diazepane-1-carbonyl)-4-fluorophenyl]methyl]-2H-phthalazin-1-one;hydrochloride |
| InChI | InChI=1S/C21H21FN4O2.ClH/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);1H |
| SMILES | C1CNCCN(C1)C(=O)C2=C(C=CC(=C2)CC3=NNC(=O)C4=CC=CC=C43)F.Cl |
| Reference | H Farmer et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature 2005, 434, 917-921.
K Ratnam and JA Low. Current Development of Clinical Inhibitors of Poly(ADP-Ribose) Polymerase in Oncology. Clin. Cancer Res. 2007, 13, 1383.
NC Turner et al. A synthetic lethal siRNA screen identifying genes mediating sensitivity to a PARP inhibitor. EMBO J. 2008, 27, 1368-1377.
T Hay et al. Poly(ADP-ribose) polymerase-1 inhibitor treatment regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin. Cancer Res. 2009, 69(9), 3850. |
