HIV RT-IN-2

HIV RT-IN-2 (Compound 10y) potently inhibits all three modes of HIV-1 RT-associated RNase H activity (internal, 3'-DNA directed, 5'-RNA directed cleavage) with IC₅₀ values of 0.65-1.5 μM and inhibits the purified HIV-1 RNase H domain fragment with an IC₅₀ of 1.3 μM^[1].
HIV RT-IN-2 inhibits HIV-1 RT RNA-dependent DNA polymerase activity with an IC₅₀ of 1.2 μM^[1].
HIV RT-IN-2 does not significantly inhibit HIV-1 integrase strand transfer activity, with an IC₅₀ greater than 100 μM^[1].
HIV RT-IN-2 (10y) (30 μM; 10 min) potently inhibits HIV-1 RT-associated RNase H activity when preincubated with RT alone (97% inhibition) or with RT and MgCl₂ (79% inhibition), but shows reduced potency (14% inhibition) when added to preformed RT-substrate complexes under substrate excess conditions^[1].
HIV RT-IN-2 (10y) (30 μM; 10 min) potently inhibits HIV-1 RT-associated RNase H activity under RT excess (virion-like) conditions, with 92% inhibition when preincubated with RT alone and 80% inhibition when added to preformed RT-substrate complexes^[1].

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