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Integrase Products

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  • Integrase Inhibitors (12)
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Catalog No. Product Name Information Product Use Citations Product Validations
E0161New Bictegravir Sodium

Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM.

S0235 Lavendustin B Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1).
S1366 BMS-707035 BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
Blood Adv, 2020, 12;4(9):1845-1858
S2001 Elvitegravir (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.
J Antimicrob Chemother, 2022, dkab498
J Virol, 2022, JVI0173021
Cell Death Discov, 2020, 6:50
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.
J Antimicrob Chemother, 2022, dkab498
J Virol, 2022, JVI0173021
Nat Commun, 2021, 12(1):5919
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.
Pharmaceutics, 2022, 14(3)615
J Antimicrob Chemother, 2022, dkab498
J Infect Dis, 2022, jiac037
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.
Molecules, 2021, 26(17)5423
Mol Cell, 2020, S1097-2765(20)30723-1
Blood Adv, 2020, 12;4(9):1845-1858
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.
Hum Mol Genet, 2020, ddaa244
S4642 Dolutegravir Sodium Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.
Pharmaceutics, 2022, 14(3)615
J Antimicrob Chemother, 2022, dkab498
J Infect Dis, 2022, jiac037
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.
J Antimicrob Chemother, 2022, dkab498
J Virol, 2022, JVI0173021
Biochem Pharmacol, 2021, 197:114901
S5911 Bictegravir Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
J Cell Biochem, 2022, 10.1002/jcb.30213
J Antimicrob Chemother, 2021, dkab276
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.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c17415
J Antimicrob Chemother, 2022, dkab498
J Antimicrob Chemother, 2021, dkab276
E0161New Bictegravir Sodium

Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM.

S0235 Lavendustin B Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1).
S1366 BMS-707035 BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
Blood Adv, 2020, 12;4(9):1845-1858
S2001 Elvitegravir (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.
J Antimicrob Chemother, 2022, dkab498
J Virol, 2022, JVI0173021
Cell Death Discov, 2020, 6:50
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.
J Antimicrob Chemother, 2022, dkab498
J Virol, 2022, JVI0173021
Nat Commun, 2021, 12(1):5919
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.
Pharmaceutics, 2022, 14(3)615
J Antimicrob Chemother, 2022, dkab498
J Infect Dis, 2022, jiac037
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.
Molecules, 2021, 26(17)5423
Mol Cell, 2020, S1097-2765(20)30723-1
Blood Adv, 2020, 12;4(9):1845-1858
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.
Hum Mol Genet, 2020, ddaa244
S4642 Dolutegravir Sodium Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.
Pharmaceutics, 2022, 14(3)615
J Antimicrob Chemother, 2022, dkab498
J Infect Dis, 2022, jiac037
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.
J Antimicrob Chemother, 2022, dkab498
J Virol, 2022, JVI0173021
Biochem Pharmacol, 2021, 197:114901
S5911 Bictegravir Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
J Cell Biochem, 2022, 10.1002/jcb.30213
J Antimicrob Chemother, 2021, dkab276
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.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c17415
J Antimicrob Chemother, 2022, dkab498
J Antimicrob Chemother, 2021, dkab276
E0161New Bictegravir Sodium

Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM.

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