Beta-Lapachone

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抑制剂描述：

产品名称：Beta-Lapachone

产品别名：见爱必信官网

英文别名：Beta-Lapachone

靶点：Topoisomerase

CAS：4707-32-8

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Beta-Lapachone是一种选择性的DNA topoisomerase I（DNA拓扑异构酶I）抑制剂，对DNA拓扑异构酶II或连接酶无抑制作用。Beta-Lapachone抑制DNA topoisomerase I诱导的DNA松弛，这种作用具有剂量依赖性。Beta-Lapachone (100 nM或更高)处理，与对照组相比，抑制95%以上Topo I DNA舒展活性。Beta-Lapachone(1-5 μM)作用于HL-60和三种前列腺癌(DU-145, PC-3, 和LNCaP)细胞，使细胞周期停滞在G0/G1期，并通过锁定Topo I在DNA上和阻止复制叉移动，而诱导细胞凋亡。

溶解性：Ethanol ：12.1 mg/mL (50 mM)
DMSO ：24.2 mg/mL (100 mM)

体外研究：

Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. Beta-Lapachone facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. In addition, beta-Lapachone inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and beta-lapachone also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. Beta-lapachone induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation.

体内研究：Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of beta-lapachone and taxol produces a synergistic induction of apoptosis. In normal and diabetic (db/db) mice, treatment of beta-lapachone results in a faster healing process than vehicle only.

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