Integrase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Integrase Products

New Integrase Products
Catalog No. Information Product Use Citations Product Validations
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.

S2001

Elvitegravir (GS-9137, JTK-303)

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

S2667

Dolutegravir (GSK1349572)

Dolutegravir (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.

S1366

BMS-707035

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

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.

S5911New

Bictegravir

Bictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.

S5245New

Raltegravir potassium

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

S7766

Cabotegravir (GSK744, GSK1265744)

Cabotegravir (GSK744, 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.

S4642

Dolutegravir Sodium

Dolutegravir sodium is a HIV integrase inhibitor with IC50 of 2.7 nM.

S4187

Salicylanilide

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

Catalog No. Information Product Use Citations Product Validations
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.

S2001

Elvitegravir (GS-9137, JTK-303)

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

S2667

Dolutegravir (GSK1349572)

Dolutegravir (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.

S1366

BMS-707035

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

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.

S5911New

Bictegravir

Bictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.

S5245New

Raltegravir potassium

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

S7766

Cabotegravir (GSK744, GSK1265744)

Cabotegravir (GSK744, 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.

S4642

Dolutegravir Sodium

Dolutegravir sodium is a HIV integrase inhibitor with IC50 of 2.7 nM.

S4187

Salicylanilide

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

Tags: Integrase activity | Integrase inhibitors mechanism | HIV Integrase inhibitor mechanism | Integrase assay | HIV Integrase assay | Integrase inhibitor drugs | HIV Integrase inhibitor drugs | Integrase inhibitor resistance testing | Integrase inhibitor review