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 (23):

Cat. No. Product Name Effect Purity
  • HY-13238
    Dolutegravir Inhibitor 99.95%
    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 99.88%
    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-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-15592
    Cabotegravir Inhibitor 98.04%
    Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.
  • 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-13238A
    Dolutegravir sodium Inhibitor 99.96%
    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 salt Inhibitor 99.96%
    Raltegravir potassium salt (MK 0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.
  • HY-18601
    (±)-BI-D Inhibitor
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
  • HY-13269
    BMS-707035 Inhibitor 99.95%
    BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM.
  • HY-18595
    BI 224436 Inhibitor ≥98.0%
    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-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-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-13305
    MK-2048 Inhibitor ≥98.0%
    MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
  • HY-10522
    HIV-1 integrase inhibitor 2 Inhibitor 99.41%
    HIV-1 integrase inhibitor 2, in the treatment of human immunodeficiency virus (HIV) infection.
  • 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.
  • HY-13025
    HIV-1 integrase inhibitor Inhibitor 98.64%
    HIV-1 integrase inhibitor is uesful for anti-HIV.
  • 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.
  • HY-108817
    HIV-1 integrase inhibitor 3 Inhibitor
    HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.
  • HY-12210
    (S)-BI-1001 Inhibitor
    (S)-BI-1001 (Compound 11) is an active S-enantiomer of BI-1001. (S)-BI-1001 exhibits antiviral potency against HIV-1 integrase with an IC50 of 28 nM, an EC50 of 450 nM and a Kd of 4.7 μM.
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