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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(S)-BI-1001
0 ImagesCat. No.: HY-12210CAS No.: 957889-73-5
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Elvitegravir-d5
0 ImagesCat. No.: HY-14740S3CAS No.: 1131640-69-1Synonyms: GS-9137-d5; JTK-303-d5; D06677-d5Elvitegravir-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.
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HIV-1 integrase inhibitor 7
0 ImagesCat. No.: HY-130760CAS No.: 204268-03-1
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Cabotegravir-d6
0 ImagesCat. No.: HY-15592S4Synonyms: GSK-1265744-d6; S/GSK1265744-d6Cabotegravir-d6 (GSK-1265744-d6) is the deuterium labeled Cabotegravir (HY-15592). 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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Averionol
0 ImagesCat. No.: HY-W876243CAS No.: 1244-78-6Averionol (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.
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D719
0 ImagesCat. No.: HY-183926CAS No.: 384361-09-5D719 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.
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HIV-1 integrase inhibitor 10
0 ImagesCat. No.: HY-150079HIV-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).
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Dolutegravir-d3
0 ImagesSynonyms: S/GSK1349572-d3Dolutegravir-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).
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HIV-1-IN-94
0 ImagesCat. No.: HY-184700CAS No.: 3124729-94-5HIV-1-IN-94 is a dual inhibitor of HIV-1 integrase (INST) and reverse transcriptase RNase H, with IC50 values of 12 μM and 0.11 μM, respectively. HIV-1-IN-94 inhibits HIV-1 replication with low cytotoxicity. HIV-1-IN-94 can be used in studies related to HIV-1 infection.
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Integrase-LEDGF/p75 allosteric inhibitor 1
0 ImagesCat. No.: HY-147653CAS No.: 1431738-14-5Integrase-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.
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HIV-1 integrase inhibitor 11
0 ImagesCat. No.: HY-W507252CAS No.: 54030-51-2
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HIV-1 integrase inhibitor 12
0 ImagesCat. No.: HY-159091HIV-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.
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Kuwanon L
0 ImagesCat. No.: HY-N18192CAS No.: 88524-65-6Kuwanon 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.
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Peruvianoside II
0 ImagesCat. No.: HY-N16888CAS No.: 450407-31-5Peruvianoside 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.
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Vanillic acid 4-O-β-D-glucopyranoside
0 ImagesCat. No.: HY-N17982CAS No.: 879627-80-2Vanillic 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.
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Bictegravir-d5
0 ImagesCat. No.: HY-17605S1Synonyms: GS-9883-d5Bictegravir-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.
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XZ426 (Standard)
0 ImagesCat. No.: HY-108818RCAS No.: 1638504-52-5
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Raltegravir (Standard)
0 ImagesCat. No.: HY-10353RCAS No.: 518048-05-0Synonyms: MK-0518 (Standard)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.
