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 (99):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-130760
    HIV-1 integrase inhibitor 7
    		Inhibitor
    HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC50 of 33.3 nM.
    HIV-1 integrase inhibitor 7
  • HY-161945
    IN-RNA-IN-2
    		Inhibitor
    IN-RNA-IN-2 (compound 1a) is an inhibitor (IC50=70 nM) of the interaction between HIV-1 integrase and the viral RNA genome. IN-RNA-IN-2 exerts its anti-HIV activity by inhibiting the viral replication process.
    IN-RNA-IN-2
  • HY-182277
    GSK-1264
    		Inhibitor
    GSK-1264 is an HIV-1 integrase inhibitor. GSK-1264 binds to a site spanning the HIV-1 integrase catalytic core domain and C-terminal domain, mediates formation of an open polymer of HIV-1 integrase dimers via inhibitor-bridged contacts between adjacent dimers. GSK-1264 disrupts late-stage HIV replication by interfering with viral particle assembly. GSK-1264 stimulates inappropriate polymerization of HIV-1 integrase. GSK-1264 can be used for the research of HIV infection.
    GSK-1264
  • HY-W876243
    Averionol
    Averionol (Compound 26) is a flavonoid compound. Averionol has no significant inhibitory activity against HIV integrase. Averionol can be used in the development of anti-HIV agents.
    Averionol
  • HY-183926
    D719
    		Inhibitor
    D719 is an HIV-1 integrase inhibitor. D719 binds to the hydrophobic pocket of HIV-1 integrase CCD dimer, disrupts interaction with LEDGF/P75, and prevents integrase nuclear translocation. D719 reduces HIV-1 p24 antigen production in acute infection of human T cells. D719 can be used for the research of HIV infection.
    D719
  • HY-150079
    HIV-1 integrase inhibitor 10
    		Inhibitor
    HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).
    HIV-1 integrase inhibitor 10
  • HY-13238S1
    Dolutegravir-d3
    		Inhibitor 99.64%
    Dolutegravir-d3 is the deuterium labeled Dolutegravir. 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-d<sub>3</sub>
  • HY-147653
    Integrase-LEDGF/p75 allosteric inhibitor 1
    		Inhibitor
    Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432.
    Integrase-LEDGF/p75 allosteric inhibitor 1
  • HY-W507252
    HIV-1 integrase inhibitor 11
    		Inhibitor
    HIV-1 integrase inhibitor 11 (compound 5) is a potent inhibitor of HIV-1 integrase, with the IC50 of 125 μM.
    HIV-1 integrase inhibitor 11
  • HY-159091
    HIV-1 integrase inhibitor 12
    		Inhibitor
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats.
    HIV-1 integrase inhibitor 12
  • HY-N18192
    Kuwanon L
    		Inhibitor
    Kuwanon L is an HIV-1 integrase (HIV-1 integrase) inhibitor, with IC50 values of 42 μM and 34 μM for LEDGF-dependent and LEDGF-independent integrase, respectively. Kuwanon L blocks the interaction between HIV-1 integrase and LEDGF/p75, with an IC50 of 22 μM. Kuwanon L inhibits HIV-1 replication in immune cells. Kuwanon L is applicable to research related to HIV-1 infection.
    Kuwanon L
  • HY-N16888
    Peruvianoside II
    		Control
    Peruvianoside II is a flavanone glucoside compound. Peruvianoside II shows no inhibitory activity against both HIV-1 reverse transcriptase and HIV-1 integrase at concentrations below 100 μM. Peruvianoside II can be extracted from the leaves of Thevetia peruviana.
    Peruvianoside II
  • HY-N17982
    Vanillic acid 4-O-β-D-glucopyranoside
    		Control
    Vanillic acid 4-O-β-D-glucopyranoside is a vanillic acid glycoside with moderate antioxidant activity. Vanillic acid 4-O-β-D-glucopyranoside scavenges DPPH free radicals and superoxide anion radicals, and inhibits AAPH-induced lipid peroxidation in the linoleic acid system. The IC50 value of Vanillic acid 4-O-β-D-glucopyranoside against HIV-1 integrase is >100 μg/mL, indicating that it is not an effective HIV-1 integrase inhibitor. Vanillic acid 4-O-β-D-glucopyranoside is isolable from the ethyl acetate extract of Gardeniae Fructus.
    Vanillic acid 4-O-β-D-glucopyranoside
  • HY-17605S1
    Bictegravir-d5
    		Inhibitor
    Bictegravir-d5 is deuterated labeled Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir-d<sub>5</sub>
  • HY-108818R
    XZ426 (Standard)
    		Inhibitor
    XZ426 (Standard) is the analytical standard of XZ426 (HY-108818). This product is intended for research and analytical applications. XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity.
    XZ426 (Standard)
  • HY-10353R
    Raltegravir (Standard)
    		Inhibitor
    Raltegravir (Standard) is the analytical standard of Raltegravir (HY-10353). This product is intended for research and analytical applications. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir (Standard)
  • HY-16907A
    GSK-364735 potassium
    		Inhibitor
    GSK-364735 potassium (S/GSK-364735 potassium) is the potassium salt form of GSK-364735 (HY-16907). GSK-364735 potassium is an antiretroviral, that inhibits the integrase of human immunodeficiency virus type 1 (HIV-1) with an IC50 of 7.8 nM.
    GSK-364735 potassium
  • HY-13238S2
    Dolutegravir-d5
    		Inhibitor
    Dolutegravir-d5 is deuterium labeled Dolutegravir. 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-d<sub>5</sub>
  • HY-15592R
    Cabotegravir (Standard)
    		Inhibitor
    Cabotegravir (Standard) is the analytical standard of Cabotegravir. This product is intended for research and analytical applications. 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 (Standard)
  • HY-14740S1
    Elvitegravir-d6
    		Inhibitor
    Elvitegravir-d6 (GS-9137-d6) is 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>6</sub>