PARP-1-IN-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells.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.Cell Proliferation Assay Cell Line:A549, HFF cellsConcentration:0, 0.1, 1, 10 μM Incubation Time:24, 48 h Result:Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells.Western Blot Analysis Cell Line:A549 cells Concentration:0, 0.1, 1, 10 μM Incubation Time:24 h Result: Reduced expression of pro-caspase-3 and phosphorylated AKT, significantly increased the expression of caspase-3 and caspase-9 protein, and enhanced expression of the cleaved PARP-1.

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Cell Cycle/DNA Damage

PARP

PARP

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684234-55-7

424.28

C22H15Cl2N3O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (196.40 mM; 超声助溶 )

Clc1ccc(cc1)-c1nn(CC(=O)Nc2cccc(Cl)c2)c(=O)c2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years