HIV-1 integrase inhibitor 8

Research use only, not for human use.

HIV-1 integrase inhibitor 8 is an inhibitor of HIV-1 integrase, a critical enzyme necessary for the integration step in HIV replication .

HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8.

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.

——

——

Microbiology/Virology

HIV

HIV Protease

——

——

1568-80-5

308.41

C21H24O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (405.30 mM; Ultrasonic )

CC1(C)CC2(CC(C)(C)c3ccc(O)cc23)c2cc(O)ccc12

——

(-20℃)

With Ice Pack

≥ 2 years