HIV Integrase Inhibitor

IN-RNA-IN-2 (compound 1a) is an inhibitor (IC₅₀=70 nM) of the interaction between HIV-1 integrase and the viral RNA genome. IN-RNA-IN-2 exerts its anti-HIV activity by inhibiting the viral replication process.

GSK-1264 is an HIV-1 integrase inhibitor. GSK-1264 binds to a site spanning the HIV-1 integrase catalytic core domain and C-terminal domain, mediates formation of an open polymer of HIV-1 integrase dimers via inhibitor-bridged contacts between adjacent dimers. GSK-1264 disrupts late-stage HIV replication by interfering with viral particle assembly. GSK-1264 stimulates inappropriate polymerization of HIV-1 integrase. GSK-1264 can be used for the research of HIV infection.

GS-9160 is a HIV-1 integrase strand transfer inhibitor with an IC₅₀ of 28 nM. GS-9160 elevates the level of HIV-1 double long terminal repeat circles and reduces integration junctions. GS-9160 exhibits selective antiviral activity against HIV-1 in cells. GS-9160 can select for integrase mutants E92V and L74M, and shows synergistic activity with other HIV-1 inhibitors. GS-9160 can be used in studies related to HIV-1 infection.

Cabotegravir-d₆ (GSK-1265744-d₆) is the deuterium labeled Cabotegravir (HY-15592). Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS.

D719 is an HIV-1 integrase inhibitor. D719 binds to the hydrophobic pocket of HIV-1 integrase CCD dimer, disrupts interaction with LEDGF/P75, and prevents integrase nuclear translocation. D719 reduces HIV-1 p24 antigen production in acute infection of human T cells. D719 can be used for the research of HIV infection.

HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC₅₀ values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).

Dolutegravir-d₃ is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM).

HIV-1-IN-94 is a dual inhibitor of HIV-1 integrase (INST) and reverse transcriptase RNase H, with IC₅₀ values of 12 μM and 0.11 μM, respectively. HIV-1-IN-94 inhibits HIV-1 replication with low cytotoxicity. HIV-1-IN-94 can be used in studies related to HIV-1 infection.

Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC₅₀ of 3.9 nM against HIV-1 recombinant molecular clone NL432.

HIV-1 integrase inhibitor 11 (compound 5) is a potent inhibitor of HIV-1 integrase, with the IC₅₀ of 125 μM.

HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC₅₀ of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC₅₀ of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats.

Kuwanon L is an HIV-1 integrase (HIV-1 integrase) inhibitor, with IC₅₀ values of 42 μM and 34 μM for LEDGF-dependent and LEDGF-independent integrase, respectively. Kuwanon L blocks the interaction between HIV-1 integrase and LEDGF/p75, with an IC₅₀ of 22 μM. Kuwanon L inhibits HIV-1 replication in immune cells. Kuwanon L is applicable to research related to HIV-1 infection.

Bictegravir-d₅ is deuterated labeled Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC₅₀ of 7.5 nM.

XZ426 (Standard) is the analytical standard of XZ426 (HY-108818). This product is intended for research and analytical applications. XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity.

Raltegravir (Standard) is the analytical standard of Raltegravir (HY-10353). This product is intended for research and analytical applications. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.

GSK-364735 potassium (S/GSK-364735 potassium) is the potassium salt form of GSK-364735 (HY-16907). GSK-364735 potassium is an antiretroviral, that inhibits the integrase of human immunodeficiency virus type 1 (HIV-1) with an IC₅₀ of 7.8 nM.

Dolutegravir-d₅ is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM).

Cabotegravir (Standard) is the analytical standard of Cabotegravir. This product is intended for research and analytical applications. Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS.

Elvitegravir-d₆ (GS-9137-d₆) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) 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, respectively.

Hyrtiosal, found in the marine sponge Hyrtios erectus, is an inhibitor of the N-terminal domain (NTD) of HIV-1 integrase (HIV-1 IN) with an IC₅₀ value of 9.60-0.86 μM. Hyrtiosal binds to the Ser17, Trp19, and Lys34 sites on the NTD of HIV-1 IN, inhibiting the binding of HIV-1 viral DNA to integrase and interfering with the formation of the pre-integrated complex of HIV-1. Hyrtiosal is promising for research of anti-HIV agents.