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 (64):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10353AS1
    Raltegravir-13C,d3 potassium
    		Inhibitor
    Raltegravir-13C,d3 potassium is 13C labeled Raltegravir potassium (HY-10353A). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir-<sup>13</sup>C,d<sub>3</sub> potassium
  • HY-15592AS
    Cabotegravir-d3 sodium
    Cabotegravir-d3 (sodium) is the deuterium labeled Cabotegravir sodium. Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltr
    Cabotegravir-d<sub>3</sub> sodium
  • HY-10353S1
    Raltegravir-d6
    		Inhibitor
    Raltegravir-d6 is a deuterated labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir-d<sub>6</sub>
  • HY-121096
    Funalenone
    		Inhibitor
    Funalenone (BMS-304245) is a MraY + MurG inhibitor with an IC50 of 25.5 μM in a MraY + MurG membrane plate assay. Funalenone inhibits Staphylococcus aureus (A15090) with an MIC of 64 μg/mL. Funalenone also inhibits MMP-1 with an IC50 of 170 μM.
    Funalenone
  • HY-N1347R
    Robinetin (Standard)
    		Inhibitor
    Robinetin (Standard) is the analytical standard of Robinetin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-P2379
    His-Cys-Lys-Phe-Trp-Trp
    		Inhibitor
    His-Cys-Lys-Phe-Trp-Trp is an inhibitor for the human immunodeficiency virus (HIV) integrase with an IC50 of 2 μM.
    His-Cys-Lys-Phe-Trp-Trp
  • 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.
    (S)-BI-1001
  • 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-N12036
    Dihydroobionin B
    		Inhibitor
    Dihydroobionin B is a potent
    Dihydroobionin B
  • 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-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)[1][2].
    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-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-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-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-W103287
    2-Hydroxyisoquinoline-1,3(2H,4H)-dione
    		Inhibitor
    Hydroxyisoquinoline-1,3(2H,4H)-dione (compound 6a) is a HIV-1 integrase (IN) and HIV-1 reverse transcriptase (RT) ribonuclease H (RNase H) inhibitor with an IC50 value of 6.32, 5.9 µM, respectively.
    2-Hydroxyisoquinoline-1,3(2H,4H)-dione