PARP1-IN-10 (compound 12c) is a highly potent and non-cytotoxic PARP1 inhibitor, displaying an in vitro IC50 value of 50.62 nM. This compound effectively induces cell cycle arrest at the G2/M phase and apoptosis, while also significantly augmenting the cytotoxic effects of temozolomide (TMZ) [1].

PARP1-IN-10 (compound 12c) (10 μM, 48 h) shows no cytotoxic effects against NCI-60 human tumor cell lines [1]. PARP1-IN-10 inhibits MDA-MB-436 cell line with an IC 50 value of 3.73 μM [1]. PARP1-IN-10 (1 and 3.73 μM, 48 h) causes cell cyle arrest at G2/M with dose-dependent manner [1]. PARP1-IN-10 (0.5 μM, 48 h) shows antiprolifetative effect of temozolomide (TMZ) about 7 times ( IC 50 = 3.64 μM) in A549 cell line compared to TMZ alone ( IC 50 =24.2 μM) [1]. Cell Cytotoxicity Assay [1] Cell Line: NCI-60 human tumor cells Concentration: 10 μM Incubation Time: 48 hours Result: Showed no toxicity. Cell Cycle Analysis [1] Cell Line: MDA-MB-436 cells Concentration: 0, 1, 3.73 μM Incubation Time: 48 hours Result: Caused cell cycle arrest at G2/M and showed apoptotic effect in dose-dependent manner. Apoptosis Analysis [1] Cell Line: A549 human lung cancer cells Concentration: 0, 0.5, 7.94 μM Incubation Time: 48 hours Result: Potentiated the antiproliferative effect of temozolomide (TMZ) 7 times compared with TMZ alone.