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 (40):

Cat. No. Product Name Effect Purity
  • 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).
  • HY-17605
    Bictegravir
    Inhibitor 99.75%
    Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
  • HY-10353
    Raltegravir
    Inhibitor 98.13%
    Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
  • HY-15592
    Cabotegravir
    Inhibitor 98.04%
    Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase 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 drugs (ARVs). Cabotegravir can be used to research AIDS.
  • 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.
  • HY-15592A
    Cabotegravir sodium
    Inhibitor 99.75%
    Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase 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 drugs (ARVs). Cabotegravir sodium can be used to research AIDS.
  • 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.
  • HY-10353B
    Raltegravir sodium
    Inhibitor
    Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
  • HY-13238A
    Dolutegravir sodium
    Inhibitor 99.88%
    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).
  • HY-10353A
    Raltegravir potassium
    Inhibitor 99.96%
    Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
  • 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.
  • 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.
  • 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).
  • 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.
  • HY-13025
    HIV-1 integrase inhibitor
    Inhibitor
    HIV-1 integrase inhibitor is uesful for anti-HIV.
  • HY-10522
    LEDGIN6
    Inhibitor 98.80%
    LEDGIN6 (CX05168) is a quinoline-based protein-protein interaction inhibitor of LEDGF/p75 and HIV integrase.
  • 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.
  • HY-N6711
    Equisetin
    Inhibitor 98.02%
    Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537. Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity. Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria. Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections.
  • HY-108935
    Lavendustin B
    Inhibitor 98.04%
    Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases.
  • HY-108820
    HIV-1 integrase inhibitor 4
    Inhibitor
    HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.