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D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells). IC50 value: 23.8 μg/ml (EC50, in MT-4 cell ), 5.03 μg/ml (EC50, in C8166 cell) Target: HIV-1 in vitro: D77 exhibits a highly specific binding affinity to HIV-1 integrase catalytic core domain.D77 induces a dramatic concentration-dependent decrease of α-galactosidase activity compared to the D77-untreated cells. D77 reveals a significant inhibition activity against the interaction of IN with IBD.

[1] Du L, et al. D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. Biochem Biophys Res Commun. 2008 Oct 10;375(1):139-144. DOI:10.1016/j.bbrc.2008.07.139