1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. HIV Integrase

HIV Integrase

HIV integrase is one of the three key enzymes of the pol gene of HIV. HIV integrase catalyzes the insertion into the genome of the infected human cell of viral DNA produced by the retrotranscription process. This unique step in the virus life cycle provides a variety of points for intervention and hence is an attractive target for the development of new therapeutics for the treatment of AIDS. HIV integrase includes HIV-1 and HIV-2 integrases.

HIV-1 integrase is a 32-kDa enzyme that carries out DNA integration in a two-step reaction. In the first step, called 3′ processing, two nucleotides are removed from each 3′ end of the viral DNA made by reverse transcription. In the next step, called DNA strand transfer, a pair of transesterification reactions integrates the ends of the viral DNA into the host genome. Integrase is comprised of three structurally and functionally distinct domains, and all three domains are required for each step of the integration reaction.

HIV Integrase Related Products (45):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13238
    Dolutegravir
    Inhibitor 99.65%
    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).
    Dolutegravir
  • HY-10353
    Raltegravir
    Inhibitor 99.53%
    Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir
  • HY-17605
    Bictegravir
    Inhibitor 99.79%
    Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir
  • HY-15592
    Cabotegravir
    Inhibitor 99.84%
    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 HIVADA, 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.
    Cabotegravir
  • HY-14740
    Elvitegravir
    Inhibitor 99.85%
    Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
    Elvitegravir
  • HY-15592S2
    Cabotegravir-d3-1
    Inhibitor
    Cabotegravir d3-1 (GSK-1265744-d3-1) is a deuterium substitute of Cabotegravir. Cabotegravir is a potent HIV integrase inhibitor used in AIDS research
    Cabotegravir-d<sub>3</sub>-1
  • HY-121096
    Funalenone
    Inhibitor
    Funalenone (BMS-304245) is a MraY + MurG inhibitor with an IC50 of 25.5 μM in a MraY + MurG membrane plate assay. Funalenone inhibits Staphylococcus aureus (A15090) with an MIC of 64 μg/mL. Funalenone also inhibits MMP-1 with an IC50 of 170 μM.
    Funalenone
  • HY-N12036
    Dihydroobionin B
    Inhibitor
    Dihydroobionin B is a potent
    Dihydroobionin B
  • HY-13238A
    Dolutegravir sodium
    Inhibitor 99.97%
    Dolutegravir sodium (S/GSK1349572 sodium) 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 sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
    Dolutegravir sodium
  • HY-N0457A
    L-Chicoric Acid
    Inhibitor 99.98%
    L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture.
    L-Chicoric Acid
  • HY-15592A
    Cabotegravir sodium
    Inhibitor 99.87%
    Cabotegravir (GSK-1265744) sodium 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 HIVADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS.
    Cabotegravir sodium
  • HY-10353A
    Raltegravir potassium
    Inhibitor 99.96%
    Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir potassium
  • HY-108818
    XZ426
    Inhibitor 99.81%
    XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity.
    XZ426
  • HY-17605A
    Bictegravir sodium
    Inhibitor 99.71%
    Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity.
    Bictegravir sodium
  • HY-13025
    HIV-1 integrase inhibitor
    Inhibitor
    HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    HIV-1 integrase inhibitor
  • HY-13269
    BMS-707035
    Inhibitor 99.50%
    BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1).
    BMS-707035
  • HY-18595
    BI 224436
    Inhibitor 99.74%
    BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
    BI 224436
  • HY-B1408
    Salicylanilide
    Inhibitor 99.90%
    Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
    Salicylanilide
  • HY-N1347
    Robinetin
    Inhibitor
    Robinetin (3,3',4',5',7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation.
    Robinetin
  • HY-18601
    (±)-BI-D
    Inhibitor 98.02%
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
    (±)-BI-D