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.
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HIV Integrase Related Products (105)
Related Products (105)
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GSK-364735 potassium
0 ImagesCat. No.: HY-16907ACAS No.: 912672-93-6Synonyms: S/GSK-364735 potassiumGSK-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.
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Dolutegravir-d5
0 ImagesCat. No.: HY-13238S2CAS No.: 2249814-82-0Synonyms: S/GSK1349572-d5Dolutegravir-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).
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Cabotegravir (Standard)
0 ImagesSynonyms: GSK-1265744 (Standard); S/GSK1265744 (Standard)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.
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Elvitegravir-d6
0 ImagesCat. No.: HY-14740S1Synonyms: GS-9137-d6; JTK-303-d6; D06677-d6Elvitegravir-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.
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Hyrtiosal
0 ImagesCat. No.: HY-N15327CAS No.: 138355-07-4Hyrtiosal, found in the marine sponge Hyrtios erectus, is an inhibitor of the N-terminal domain (NTD) of HIV-1 integrase (HIV-1 IN) with an IC50 value of 9.60-0.86 μM. Hyrtiosal binds to the Ser17, Trp19, and Lys34 sites on the NTD of HIV-1 IN, inhibiting the binding of HIV-1 viral DNA to integrase and interfering with the formation of the pre-integrated complex of HIV-1. Hyrtiosal is promising for research of anti-HIV agents.
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Salicylanilide (Standard)
0 ImagesSalicylanilide (Standard) is the analytical standard of Salicylanilide. This product is intended for research and analytical applications. Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
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MK-0536
0 ImagesCat. No.: HY-123883CAS No.: 865298-81-3MK-0536 is a highly potent HIV-1 integrase inhibitor that effectively suppresses the replication of wild-type viruses. MK-0536 retains significant antiviral activity against multiple key drug-resistant mutants such as Y143R and N155H, and shows no toxicity to uninfected cells. MK-0536 selectively blocks the strand transfer reaction of integrase by chelating magnesium ions at the active site and interacting with viral DNA and enzyme residues. MK-0536 is applicable to the study of HIV infection mechanisms.
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Herbacitrin
0 ImagesCat. No.: HY-N15438CAS No.: 35815-07-7Herbacitrin is a HIV-1 reverse transcriptase and integrase inhibitor with IC50 values of 21.5 μM and 2.15 μM, respectively. Herbacitrin inhibits the growth of normal mouse embryonic cells, hybridoma HF cells, and ras/myc-transformed SFME cells, regulates the growth of ras-transformed SFME cells, and exhibits cytotoxic activity against hybridoma HF cells. Herbacitrin can be used in studies related to HIV-1 infection.
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L-731988
0 ImagesCat. No.: HY-182678CAS No.: 251922-77-7L-731988 is an inhibitor targeting HIV-1 integrase. L-731988 inhibits HIV-1 replication by blocking integrase function. L-731988 exhibits ED50 values ranging from 0.5 μM to 3.14 μM against various HIV-1 isolates. L-731988 can be used for the research of human immunodeficiency virus type 1 (HIV-1) infection.
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L-870812
0 ImagesCat. No.: HY-122256CAS No.: 410545-90-3
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Robinetin (Standard)
0 ImagesRobinetin (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.
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Raltegravir-d4 potassium
0 ImagesCat. No.: HY-10353AS2Synonyms: MK 0518-d4 potassiumRaltegravir-d4 (potassium) (MK 0518-d4 (potassium)) is deuterium labeled Raltegravir (potassium). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
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LEDGIN6 (Standard)
0 ImagesCat. No.: HY-10522RCAS No.: 957890-42-5Synonyms: CX05168 (Standard); CX04328 (Standard)LEDGIN6 (Standard) is the analytical standard of LEDGIN6 (HY-10522). This product is intended for research and analytical applications. LEDGIN6 (CX05168) is a quinoline-based protein-protein interaction inhibitor of LEDGF/p75 and HIV integrase.
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Raltegravir potassium (Standard)
0 ImagesCat. No.: HY-10353ARCAS No.: 871038-72-1Synonyms: MK 0518 potassium (Standard)Raltegravir (potassium) (Standard) is the analytical standard of Raltegravir (potassium). This product is intended for research and analytical applications. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
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BMS-707035 (Standard)
0 ImagesBMS-707035 (Standard) is the analytical standard of BMS-707035. This product is intended for research and analytical applications. 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).
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5-CITEP
0 ImagesCat. No.: HY-50693CAS No.: 900779-63-75 CITEP is a potent HIV integrase inhibitor; its IC50s by multiple MIA and MPA are 2.
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Bictegravir-d7
0 ImagesCat. No.: HY-17605S4CAS No.: 2171092-56-9Synonyms: GS-9883-d7Bictegravir-d7 (GS-9883-d7) is deuterium labeled Bictegravir. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
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Elvitegravir-13C6
0 ImagesCat. No.: HY-14740S2Synonyms: GS-9137-13C6 ; JTK-303-13C6 ; D06677-13C6Elvitegravir-13C6 (GS-9137-13C6) is 13C 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.
