APE1-IN-2,2923433-95-6

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APE1-IN-2

CAS No. : 2923433-95-6

MCE 国际站：APE1-IN-2

产品活性：APE1-IN-2 (compound AP1) 是一种 Pt(IV) 前体，靶向一个关键的 BER 蛋白，无嘌呤/无嘧啶核酸内切酶 1 (APE1)。APE1-IN-2 具有抗癌活性。APE1-IN-2 可诱导细胞内铂积累，激活 DNA 损伤反应和凋亡 (apoptosis) 信号。

研究领域：Apoptosis

作用靶点：Apoptosis  |  MDM-2/p53

In Vitro: APE1-IN-2 (compound AP1) can strongly inhibit the growth of malignant cells, including Cisplatin-resistant cancer cells, with up to 18.11 times inhibition compared with Cisplatin (HY-17394).
APE1-IN-2 (500 nM, 24 h) arrests the cell cycle in A549 and MCF7 cells.
APE1-IN-2 (10 μM, 24 h) induces p53-dependent apoptosis in A549 cells.
APE1-IN-2 (0-250 μM, 72 h) inhibits AP-cutting activity with an IC₅₀ of 45.14 ± 17.37 μM.
APE1-IN-2 can directly inhibit the AP endonuclease activity of APE1, leading to an interruption of miRNA processing and upregulation of the tumor suppressor PTEN.

In Vivo: APE1-IN-2 (compound AP1) (2 mg/kg, IP, once every 3 days for 15 days) exhibits an antitumor effect on the A549 xenograft model.

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