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 Mn 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.
分子式
C21H28O2
分子量
308.41
CAS号
1568-80-5
运输条件
Room temperature in continental US; may vary elsewhere.