GS-9160

GS-9160 (range; 30 min) potently inhibits purified HIV-1 integrase strand transfer activity with an IC₅₀ of 28 nM^[1].
GS-9160 (5 days) potently inhibits HIV-1 IIIb replication in MT-2 cells with an EC₅₀ of 2.1 nM and a selectivity index of 1,905^[1].
GS-9160 (5 days) potently inhibits HIV-1 IIIb replication in MT-4 cells with an EC₅₀ of 0.7 nM and a selectivity index of 457^[1].
GS-9160 (5 days) potently inhibits HIV-1 BaL replication in primary human CD4-positive T lymphocytes with an EC₅₀ of 1.5 nM and a selectivity index of 2,667^[1].
GS-9160 (tested doses; period sufficient for viral replication and circle formation) blocks HIV-1 integration in SupT1 cells, as evidenced by a 1.9-fold increase in 2-LTR circle levels, with a cytotoxicity CC₅₀ of 600 nM^[1].
GS-9160 (48 h) specifically inhibits HIV-1 integration in SupT1 cells, reducing integration junctions with an EC₅₀ of 0.9 nM without affecting late reverse transcription product accumulation^[1].
GS-9160 potently inhibits HIV replication in vitro, though its activity is reduced in human serum, and it selects for HIV-1 integrase mutations integrase^E92V and integrase^L74M that are shared with other integrase strand transfer inhibitors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.