Home Microbiology Integrase

Integrase inhibitors

Retroviral integration is promoted by the viral integrase (IN) enzyme, which enters the cell as a component of the virion particle. Integrase enables retrovirus genetic material to be integrated into the host chromosome. It is essential to retrovirus replication. Integrase catalyzes two spatially and temporally distinct reactions within the context of the preintegration complex (PIC), a large structure derived from the virus core. The integrase inhibitors provide a novel target for antiretroviral therapy.

Other Microbiology Related Inhibitors

Reverse Transcriptase Anti-infection Ribosomal Peptidyl Transferase COVID-19 3C-Like Protease β-lactamase Parasite Neuraminidase CMV Fungal

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S2667 GSK1349572 (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.
Nucleic Acids Res, 2025, 53(10)gkaf449
Immunity, 2024, 57(12):2928-2944.e6
Lung Cancer, 2024, 15:55-67
Verified customer review of GSK1349572 (Dolutegravir)
S7766 GSK1265744 (Cabotegravir) 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.
Biomed Pharmacother, 2025, 184:117925
Cancer Lett, 2024, 588:216813
Nat Commun, 2023, 14(1):708
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.
J Clin Invest, 2025, 135(16)e187663
EBioMedicine, 2025, 122:106004
EMBO Mol Med, 2025, 10.1038/s44321-025-00255-x
Verified customer review of Raltegravir
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
Verified customer review of Elvitegravir
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.
PLoS Pathog, 2024, 20(3):e1011716
Cells, 2022, 11(11)1841
J Virol, 2022, JVI0173021
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
Verified customer review of Dolutegravir Sodium
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
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

Signaling Pathway Map