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

HIV Integrase

HIV Integrase

Related Products

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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 (96):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13238
    Dolutegravir
    		Inhibitor 99.94%
    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 99.82%
    Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir
  • 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-17605
    Bictegravir
    		Inhibitor 99.93%
    Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir
  • 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-185448
    HIV RT-IN-1
    		Inhibitor
    HIV RT-IN-1 is an inhibitor of HIV integrase and HIV reverse transcriptase-associated ribonuclease H. HIV RT-IN-1 is applicable to research related to HIV-1 infection.
    HIV RT-IN-1
  • HY-178833
    CNI-H0294 hydrochloride
    		Inhibitor
    CNI-H0294 hydrochloride is a selective HIV-1 integrase inhibitor. CNI-H0294 hydrochloride is promising for research of HIV-associated central nervous system diseases.
    CNI-H0294 hydrochloride
  • HY-14740S3
    Elvitegravir-d5
    		Inhibitor
    Elvitegravir-d5 (GS-9137-d5; JTK-303-d5; D06677-d5) is the deuterium labeled Elvitegravir. 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-d<sub>5</sub>
  • HY-I0096
    Indole-2-carboxylic acid
    		Inhibitor 99.86%
    Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection.
    Indole-2-carboxylic acid
  • HY-N0457A
    L-Chicoric Acid
    		Inhibitor 99.85%
    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-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-10353A
    Raltegravir potassium
    		Inhibitor 99.96%
    Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir potassium
  • HY-N1347
    Robinetin
    		Inhibitor 98.15%
    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-18257
    Rolitetracycline
    		Inhibitor ≥98.0%
    Rolitetracycline is a highly soluble, broad-spectrum antibiotic derived from tetracycline. Rolitetracycline binds to and stabilizes bovine serum albumin, and also inhibits HIV-1 integrase, blocks Aβ fibril formation and suppresses dengue virus proliferation. Rolitetracycline mediates the inhibition of Aβ fibrils via a specific three-dimensional pharmacophore conformation, and exerts bacteriostatic and bactericidal activities. Rolitetracycline acts synergistically with Penicillin G (HY-N7139) or Cephalothin (HY-B1275A) to alter the effects on microbial growth. Rolitetracycline serves as an important tool compound for the study of bacterial infections (urinary tract infections, sepsis), HIV-1 and dengue virus infections, as well as Alzheimer's disease.
    Rolitetracycline
  • HY-W010937
    1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide
    		Inhibitor 99.91%
    1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide (BMIM-TFSI; BMI-TFSI) is an HIV-1 integrase inhibitor. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide weakly inhibits recombinant HIV-1 integrase 3'-processing or strand transfer activity. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide can be used for the research of HIV-1.
    1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide
  • HY-N6711
    Equisetin
    		Inhibitor 99.40%
    Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects.
    Equisetin
  • 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-18595
    BI 224436
    		Inhibitor 98.42%
    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-17605A
    Bictegravir sodium
    		Inhibitor 99.62%
    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-130000
    Pirmitegravir
    		Inhibitor 99.79%
    Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.
    Pirmitegravir