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

HIV Integrase

HIV Integrase

Related Products

PDF 0.49 MB

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 (65):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13238
    Dolutegravir
    		Inhibitor 99.98%
    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 99.93%
    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 99.91%
    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 99.90%
    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-12108
    S 1360
    		Inhibitor
    S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase ( IC50: 20 nM). The EC50, and CC50 of S 1360 in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants.
    S 1360
  • HY-159092
    HIV-1 integrase inhibitor 13
    		Inhibitor
    HIV-1 integrase inhibitor 13 (Compound 15) is an inhibitor for HIV-1 integrase with an IC50 of 1.8 nM. HIV-1 integrase inhibitor 13 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 21 and 580 nM, respectively.
    HIV-1 integrase inhibitor 13
  • HY-16907
    GSK-364735
    		Inhibitor
    GSK-364735 is a potent antiretroviral agent against human immunodeficiency virus type 1 (HIV-1) and serves as an integrase inhibitor with an IC50 of 8 ± 2 nM. GSK-364735 can be utilized in antiviral research.
    GSK-364735
  • 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-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-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-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-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-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-10522
    LEDGIN6
    		Inhibitor 98.80%
    LEDGIN6 (CX05168) is a quinoline-based protein-protein interaction inhibitor of LEDGF/p75 and HIV integrase.
    LEDGIN6
  • HY-B1408
    Salicylanilide
    		Inhibitor 99.20%
    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-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    HIV-1 integrase inhibitor
  • HY-N6711
    Equisetin
    		Inhibitor 99.40%
    Equisetin is an N-methylserine-derived acyltramic acid isolated from the terrestrial fungus Fusarium equiseti NRRL 5537. As a tetrad-containing natural product, it has antibacterial and antiviral activities, inhibiting the growth of Gram-positive bacteria and HIV-1 integrase activity, but not Gram-negative bacteria. Equisetin is a quorum sensing inhibitor (QSI) that attenuates the QS-regulated virulence phenotype in Pseudomonas aeruginosa without affecting bacterial growth, and is a leading compound for studying Pseudomonas aeruginosa infection. In addition, equisetin inhibits the enzymatic activity of 11b-hydroxysteroid dehydrogenase type 1 (11b-HSD1) without affecting food intake, blood pressure, or heart rate, exerting anti-obesity effects on adipose tissue.
    Equisetin