产品
编 号:F187124
分子式:C21H24O2
分子量:308.41
产品类型
结构图
CAS No: 1568-80-5
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产品详情
生物活性:
HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8.
体外研究:
HIV-1 integrase inhibitor 8 is against 3′-processing (TC) and strand-transfer (ST) activities in the presence of Mn2+ as the cationic cofactor by gel assay with IC50 values of 275 μM and 200 μM, respectively. It inhibits the strand-transfer (ST) activity with an IC50 value of 200 μM.The DNA relaxation activity of MCV topoisomerase is monitored by gel electrophoresis, while DNA cleavage and religation activities were monitored using a microtiter assay. HIV-1 integrase inhibitor 8 inhibits MCV topoisomerase and DNA religation with IC50 values of 500 μM and 200 μM, respectively. This result demonstrates that compound 8 is inactive against topoisomerase in both assays. HIV-1 integrase inhibitor 8 induces cell cytotoxicity and yields a LD50 (dose at which the signal is reduced 50% due to cell death) of 20 μM in HeLa cells.