PARP-1-IN-2

• CAT Number: I043539
• CAS Number: 684234-55-7
• Molecular Formula: C22H15Cl2N3O2
• Molecular Weight: 424.28
• Purity: ≥95%
• Synonyms: N-(3-chlorophenyl)-2-[4-(4-chlorophenyl)-1-oxophthalazin-2-yl]acetamide
• InChI: InChI=1S/C22H15Cl2N3O2/c23-15-10-8-14(9-11-15)21-18-6-1-2-7-19(18)22(29)27(26-21)13-20(28)25-17-5-3-4-16(24)12-17/h1-12H,13H2,(H,25,28)
• InChIKey: ASIIOGZHCMSESG-UHFFFAOYSA-N
• SMILES: C1=CC=C2C(=C1)C(=NN(C2=O)CC(=O)NC3=CC(=CC=C3)Cl)C4=CC=C(C=C4)Cl

PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis[1].
PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 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].

Reference

[1]. Almahli H, et al. Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer. Bioorg Chem. 2018 Apr;77:443-456.
 [Content Brief]