产品名称

Beta-Lapachone

一般描述

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase.

别 称

β-Lapachone, ARQ-501, 2,2-dimethyl-3,4-dihydrobenzo[h]chromene-5,6-dione

纯 度

≥98.5%(HPLC)

CAS NO.

4707-32-8

分子式

C¹⁵H¹⁴O³

分子量

242.27

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25°C)

DMSO

≥25mg/ml

乙醇

≥5mg/ml

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Lapachone is a poorly soluble, ortho-naphthoquinone with potential antineoplastic and radiosensitizing activity. Beta-lapachone (b-lap) is bioactivated by NAD(P)H:quinone oxidoreductase-1(NQO1), creating a futile oxidoreduction that generates high levels of superoxide. In turn, the highly reactive oxygen species (ROS) interact with DNA, thereby causing single-strand DNA breaks and calcium release from endoplasmic reticulum (ER) stores. Eventually, the extensive DNA damage causes hyperactivation of poly(ADP-ribose) polymerase-1 (PARP-1), an enzyme facilitating DNA repair, accompanied by rapid depletion of NAD₊/ATP nucleotide levels. As a result, a caspase-independent and ER-stress induced mu-calpain-mediated cell death occurs in NQO1-overexpressing tumor cells. NQO1, a flavoprotein and two-electron oxidoreductase, is overexpressed in a variety of tumors.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov