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 (99):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P2259
    TAT-GluA2 3Y
    99.93%
    TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction.
    TAT-GluA2 3Y
  • HY-10522
    LEDGIN6
    Inhibitor 99.62%
    LEDGIN6 (CX05168) is a quinoline-based protein-protein interaction inhibitor of LEDGF/p75 and HIV integrase.
    LEDGIN6
  • HY-18601
    (±)-BI-D
    Inhibitor 98.06%
    (±)-BI-D is a potent ALLINI (allosteric integrase inhibitor). (±)-BI-D binds integrase at the LEDGF/p75 binding site. (±)-BI-D inhibits HIV-Luc infection in cells (IC50: 0.16 μM in Psip1 knockout E9 mouse embryonic fibroblasts, 2.9 μM in wild-type E9 mouse embryonic fibroblasts).
    (±)-BI-D
  • HY-B1408
    Salicylanilide
    Inhibitor 98.14%
    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-108818
    XZ426
    Inhibitor 99.81%
    XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity.
    XZ426
  • HY-N16050
    Ethyl salvianolate A
    Inhibitor
    Ethyl salvianolate A (Ethyl salvionolate A) is an anti-HIV-1 compound that can be extracted from the roots of Salvia yunnanensis. Ethyl salvianolate A inhibits P24 antigen in HIV-1 infected MT-4 cell cultures (EC50: 1.44 μg/mL). Ethyl salvianolate A inhibits HIV-1 replicative enzymes, with IC50s of 56.38 μM (Reverse transcriptase), 12.03 μM (Protease), 14.54 μM (Integrase), respectively.
    Ethyl salvianolate A
  • HY-153094
    BDM-2
    Inhibitor 99.09%
    BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity.
    BDM-2
  • HY-108935
    Lavendustin B
    Inhibitor 98.02%
    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.
    Lavendustin B
  • HY-123572
    Bis-T-23
    Inhibitor
    Bis-T-23 (AG1717), tyrphostin derivative, is an HIV-I integrase inhibitor. Bis-T-23 can promote actin-dependent dynamin oligomerization. Bis-T-23 can be used for the research of HIV and chronic kidney diseases (CKD).
    Bis-T-23
  • 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.
    HIV-1 integrase inhibitor 4
  • 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.
    HIV-1 integrase inhibitor 3
  • HY-15592S1
    Cabotegravir-d5
    Inhibitor 99.31%
    Cabotegravir-d5 is deuterium labeled Cabotegravir.
    Cabotegravir-d<sub>5</sub>
  • HY-107485
    HIV-1 integrase inhibitor 8
    Inhibitor 99.88%
    HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8.
    HIV-1 integrase inhibitor 8
  • 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-17605AR
    Bictegravir sodium (Standard)
    Inhibitor
    Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. 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 (Standard)
  • HY-13305
    MK-2048
    Inhibitor 99.01%
    MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.
    MK-2048
  • HY-13269
    BMS-707035
    Inhibitor 99.99%
    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-14740R
    Elvitegravir (Standard)
    Inhibitor
    Elvitegravir (Standard) is the analytical standard of Elvitegravir. This product is intended for research and analytical applications. 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 (Standard)
  • HY-13238R
    Dolutegravir (Standard)
    Inhibitor
    Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0457AR
    L-Chicoric Acid (Standard)
    Inhibitor
    L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. 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 (Standard)