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Integrase

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Integrase Products

All (14)
Integrase Inhibitors (14)
New Integrase Products

Catalog No.	Product Name	Information	Product Use Citations
S2005	Raltegravir	Raltegravir 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.	Clin Immunol, 2024, 260:109915 Front Cell Infect Microbiol, 2024, 14:1334126 Lung Cancer, 2024, 15:55-67
S2001	Elvitegravir	Elvitegravir 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.	Lung Cancer, 2024, 15:55-67 Antimicrob Agents Chemother, 2023, 67(7):e0046223 Sci Rep, 2023, 13(1):4594
S2667	Dolutegravir	Dolutegravir 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.	Lung Cancer, 2024, 15:55-67 Antimicrob Agents Chemother, 2023, 67(7):e0046223 Cell Rep Methods, 2023, 3(4):100443
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.	Cancer Lett, 2024, 588:216813 Nat Commun, 2023, 14(1):708 Pharmaceutics, 2023, 15(5)1487
S5245	Raltegravir potassium	Raltegravir Potassium(MK-0518 potassium) is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.	Cells, 2022, 11(11)1841 J Virol, 2022, JVI0173021 J Antimicrob Chemother, 2022, dkab498
S4642	Dolutegravir Sodium	Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.	J Infect Dis, 2022, jiac037 Cells, 2022, 11(11)1841 J Virol, 2022, JVI0173021
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
S5911	Bictegravir	Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.	PNAS Nexus, 2024, 3(1):pgad446 Cells, 2022, 11(11)1841 Int J Mol Sci, 2022, 23(23)15380
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
E0161	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.	Cells, 2022, 11(11)1841
S4187	Salicylanilide	Salicylanilides (WR10019,2-Hydroxybenzanilide) 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
E0459	Robinetin	Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency.
E4468	Cabotegravir Sodium	Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor. It also inhibits organic anion transporter 1/3 (OAT1/OAT3) with IC50 of 0.41 μM and 0.81 μM for OAT3 and OAT1, respectively.
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).
S2005	Raltegravir	Raltegravir 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.	Clin Immunol, 2024, 260:109915 Front Cell Infect Microbiol, 2024, 14:1334126 Lung Cancer, 2024, 15:55-67
S2001	Elvitegravir	Elvitegravir 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.	Lung Cancer, 2024, 15:55-67 Antimicrob Agents Chemother, 2023, 67(7):e0046223 Sci Rep, 2023, 13(1):4594
S2667	Dolutegravir	Dolutegravir 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.	Lung Cancer, 2024, 15:55-67 Antimicrob Agents Chemother, 2023, 67(7):e0046223 Cell Rep Methods, 2023, 3(4):100443
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.	Cancer Lett, 2024, 588:216813 Nat Commun, 2023, 14(1):708 Pharmaceutics, 2023, 15(5)1487
S5245	Raltegravir potassium	Raltegravir Potassium(MK-0518 potassium) is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.	Cells, 2022, 11(11)1841 J Virol, 2022, JVI0173021 J Antimicrob Chemother, 2022, dkab498
S4642	Dolutegravir Sodium	Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.	J Infect Dis, 2022, jiac037 Cells, 2022, 11(11)1841 J Virol, 2022, JVI0173021
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
S5911	Bictegravir	Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.	PNAS Nexus, 2024, 3(1):pgad446 Cells, 2022, 11(11)1841 Int J Mol Sci, 2022, 23(23)15380
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
E0161	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.	Cells, 2022, 11(11)1841
S4187	Salicylanilide	Salicylanilides (WR10019,2-Hydroxybenzanilide) 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
E0459	Robinetin	Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency.
E4468	Cabotegravir Sodium	Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor. It also inhibits organic anion transporter 1/3 (OAT1/OAT3) with IC50 of 0.41 μM and 0.81 μM for OAT3 and OAT1, respectively.
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).

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