| Description | PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells. |
| In vitro | PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) significantly anti-proliferative activity against A549 cells and didn’t display any significant cytotoxicity on HFF cells.[1] PARP-1-IN-2 (0-10 μM, 24 h) decreases the expression of pro-caspase-3 and phosphorylated AKT increases the expression of caspase-3, caspase-9 protein, and the cleaved PARP-1.[1] |
| Target activity | PARP1:149 ± 11.0 nM |
| molecular weight | 424.28 |
| Molecular formula | C22H15Cl2N3O2 |
| CAS | 684234-55-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 9 mg/mL (21.21 mM), Sonication is recommended. |
| References | 1. Almahli H, et al. Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer. Bioorg Chem. 2018;77:443-456. |