KU-0058948

**KU-0058948** is a potent and specific small molecule inhibitor targeting **poly(ADP-ribose) polymerase 1 (PARP1)** and **PARP3**, both enzymes involved in DNA repair[1][3][7]. Its **IC50 for PARP1 is 3.4 nM**, and it is among the strongest inhibitors of PARP3 reported[1][3]. KU-0058948 is studied as a tool compound for investigating DNA repair mechanisms and potential anti-cancer therapeutic strategies, particularly exploiting synthetic lethality in **BRCA-mutated cells**[6]. Preclinical data show it induces cell cycle arrest or apoptosis in BRCA-deficient cancer cells and has demonstrated enhanced cytotoxicity compared to cisplatin in these contexts[6]. Developed by The Institute of Cancer Research (Royal Cancer Hospital) and KuDOS Pharmaceuticals, its primary therapeutic indications are **cancer, especially ovarian and endometrial carcinoma**[5][7].

Other names

4-[3-(1,4-diazepan-1-ylcarbonyl)-4-fluorobenzyl]phthalazin-1(2H)-one4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one4-[3-([1,4]diazepane-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-oneHomopiperazine analogue 14HGEPGGJUGUMFHT-UHFFFAOYSA-N