PARP1-IN-2 (化合物 11g) 是一种有效的可透过血脑屏障的 PARP1 抑制剂，其 IC50 值为 149 nM。PARP1-IN-2 对人肺腺癌上皮细胞系 A549 具有显著的抗增殖活性。PARP1-IN-2 可诱导 A549 细胞凋亡。
货号:ajcx37890
CAS:684234-55-7
分子式:C22H15Cl2N3O2
分子量：424.28
溶解度:DMSO : 83.33 mg/mL (196.40 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.