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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Dolutegravir (Standard)
0 ImagesSynonyms: S/GSK1349572 (Standard)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).
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L-Chicoric Acid (Standard)
0 ImagesSynonyms: (-)-Chicoric acid (Standard); trans-Caffeoyltartaric acid (Standard)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.
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Raltegravir sodium
0 ImagesCat. No.: HY-10353BCAS No.: 1292804-07-9Synonyms: MK 0518 sodiumRaltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
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GSK3739936
0 ImagesCat. No.: HY-150080CAS No.: 1803444-21-4Synonyms: BMS-986180GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability.
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Raltegravir-d3 potassium
0 ImagesCat. No.: HY-10353ASCAS No.: 1246816-98-7Synonyms: MK 0518-d3 potassiumRaltegravir-d3 (potassium) is the deuterium labeled Raltegravir potassium. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
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S 1360
0 ImagesCat. No.: HY-12108CAS No.: 280571-30-4S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase ( IC50: 20 nM). The EC50, and CC50 of S 1360 in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants.
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Raltegravir-d4
0 ImagesCat. No.: HY-10353SCAS No.: 2712343-38-7Raltegravir-d4 is deuterium labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
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Elvitegravir-d8
0 ImagesCat. No.: HY-14740SSynonyms: GS-9137-d8; JTK-303-d8; D06677-d8Elvitegravir-d8 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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Cabotegravir-d3-1
0 ImagesCat. No.: HY-15592S2Synonyms: GSK-1265744-d3-1; S/GSK1265744-d3-1Cabotegravir d3-1 (GSK-1265744-d3-1) is a deuterium substitute of Cabotegravir. Cabotegravir is a potent HIV integrase inhibitor used in AIDS research
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GSK3839919A
0 ImagesCat. No.: HY-153247CAS No.: 2081127-77-5GSK3839919A is a potent and allosteric HIV-1integrase inhibitor.
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Lepetegravir
0 ImagesCat. No.: HY-177098CAS No.: 2808219-64-7Lepetegravir (Example 24) is a HIV integrase inhibitor. Lepetegravir has antiviral effects (EC50: 0.98 nM in MT-4 cells).
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Bictegravir-d4
0 ImagesCat. No.: HY-17605S2Synonyms: GS-9883-d4Bictegravir-d4 is a deuterium of 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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Raltegravir-13C,d3 potassium
0 ImagesCat. No.: HY-10353AS1Synonyms: MK-0518-13C,d3 potassiumRaltegravir-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.
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Cabotegravir-d3 sodium
0 ImagesCat. No.: HY-15592ASSynonyms: GSK-1265744-d3 sodium; S/GSK1265744-d3 sodiumCabotegravir-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
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Raltegravir-d6
0 ImagesCat. No.: HY-10353S1CAS No.: 1100750-98-8Synonyms: MK-0518-d6Raltegravir-d6 is a deuterated labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
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Funalenone
0 ImagesCat. No.: HY-121096CAS No.: 259728-61-5Synonyms: BMS-304245Funalenone (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.
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CNI-H0294 hydrochloride
0 ImagesCat. No.: HY-178833CAS No.: 180740-99-2CNI-H0294 hydrochloride is a selective HIV-1 integrase inhibitor. CNI-H0294 hydrochloride is promising for research of HIV-associated central nervous system diseases.
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His-Cys-Lys-Phe-Trp-Trp
0 ImagesCat. No.: HY-P2379CAS No.: 172546-75-7His-Cys-Lys-Phe-Trp-Trp is an inhibitor for the human immunodeficiency virus (HIV) integrase with an IC50 of 2 μM.
