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Integrase Products

All (12)
Integrase Inhibitors (12)
New Integrase Products

Catalog No.	Product Name	Information	Product Use Citations
E0161^New	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.	Cell Death Discov, 2020, 6:50 J Virol, 2019, 93(9) JCI Insight, 2019, 4(12)
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.	Nat Commun, 2021, 12(1):5919 Proc Natl Acad Sci U S A, 2021, 118(10)e2005568118 PLoS Pathog, 2021, 17(5):e1009577
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.	Int J Pharm, 2021, 605:120844 Int J Pharm X, 2021, 3:100068 Proc Natl Acad Sci U S A, 2020, 117(7):3704-3710
S2765	MK-2048	MK-2048 is a potent inhibitor of integrase (IN) and IN_R263K 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.	Blood Adv, 2020, 12;4(9):1845-1858 J Virol, 2019, 93(9) PLoS Pathog, 2016, 12(8):e1005860
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.	Elife, 2018, 7e36245 PLoS Pathog, 2018, AIDS Res Hum Retroviruses, 2018, 34(9):769-777
S5911	Bictegravir	Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.	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.	J Antimicrob Chemother, 2021, dkab276 Blood Adv, 2020, 12;4(9):1845-1858 Clin Infect Dis, 2019, 69(4):657-667
E0161^New	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.	Cell Death Discov, 2020, 6:50 J Virol, 2019, 93(9) JCI Insight, 2019, 4(12)
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.	Nat Commun, 2021, 12(1):5919 Proc Natl Acad Sci U S A, 2021, 118(10)e2005568118 PLoS Pathog, 2021, 17(5):e1009577
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.	Int J Pharm, 2021, 605:120844 Int J Pharm X, 2021, 3:100068 Proc Natl Acad Sci U S A, 2020, 117(7):3704-3710
S2765	MK-2048	MK-2048 is a potent inhibitor of integrase (IN) and IN_R263K 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.	Blood Adv, 2020, 12;4(9):1845-1858 J Virol, 2019, 93(9) PLoS Pathog, 2016, 12(8):e1005860
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.	Elife, 2018, 7e36245 PLoS Pathog, 2018, AIDS Res Hum Retroviruses, 2018, 34(9):769-777
S5911	Bictegravir	Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.	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.	J Antimicrob Chemother, 2021, dkab276 Blood Adv, 2020, 12;4(9):1845-1858 Clin Infect Dis, 2019, 69(4):657-667
E0161^New	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.