HIV-Integrase Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S2765 MK-2048

MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.

Selective Integrase, IC50: 2.6 nM; Integrase (R263K), IC50: 1.5 nM
S2667 Dolutegravir (GSK1349572)

Dolutegravir (GSK1349572, S/GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

Selective HIV integrase, IC50: 2.7 nM
S4642 Dolutegravir Sodium

Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.

Selective HIV integrase, IC50: 2.7 nM
S2005 Raltegravir (MK-0518)

Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.

Selective Integrase (WT PFV), IC50: 90 nM; Integrase (S217Q PFV), IC50: 40 nM
S5245 Raltegravir potassium

Raltegravir Potassium is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.

Selective
S7766 Cabotegravir (GSK1265744)

Cabotegravir (GSK744, GSK1265744, S/GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.

Selective
S4187 Salicylanilide

Salicylanilides (WR10019) are a group of compounds with a wide range of biological activities including antiviral potency, antibacterial (including antimycobacterial) and antifungal activities.

Selective