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 관련 제품 (105)
관련 제품 (105)
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Dolutegravir
0 ImagesSynonyms: S/GSK1349572Dolutegravir (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
0 ImagesSynonyms: GSK-1265744; S/GSK1265744Cabotegravir (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
0 ImagesSynonyms: GS-9137; JTK-303; D06677Elvitegravir (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 RT-IN-1
0 ImagesCat. No.: HY-185448CAS No.: 1246741-36-5HIV RT-IN-1 is an inhibitor of HIV integrase and HIV reverse transcriptase-associated ribonuclease H. HIV RT-IN-1 is applicable to research related to HIV-1 infection.
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GSK-1264
0 ImagesCat. No.: HY-182277CAS No.: 1392118-63-6GSK-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.
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GS-9160
0 ImagesCat. No.: HY-184318CAS No.: 915407-80-6GS-9160 is a HIV-1 integrase strand transfer inhibitor with an IC50 of 28 nM. GS-9160 elevates the level of HIV-1 double long terminal repeat circles and reduces integration junctions. GS-9160 exhibits selective antiviral activity against HIV-1 in cells. GS-9160 can select for integrase mutants E92V and L74M, and shows synergistic activity with other HIV-1 inhibitors. GS-9160 can be used in studies related to HIV-1 infection.
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Indole-2-carboxylic acid
0 ImagesIndole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection.
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L-Chicoric Acid
0 ImagesSynonyms: (-)-Chicoric acid; trans-Caffeoyltartaric acid
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Robinetin
0 ImagesRobinetin (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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Rolitetracycline
0 ImagesRolitetracycline is a highly soluble, broad-spectrum antibiotic derived from tetracycline. Rolitetracycline binds to and stabilizes bovine serum albumin, and also inhibits HIV-1 integrase, blocks Aβ fibril formation and suppresses dengue virus proliferation. Rolitetracycline mediates the inhibition of Aβ fibrils via a specific three-dimensional pharmacophore conformation, and exerts bacteriostatic and bactericidal activities. Rolitetracycline acts synergistically with Penicillin G (HY-N7139) or Cephalothin (HY-B1275A) to alter the effects on microbial growth. Rolitetracycline serves as an important tool compound for the study of bacterial infections (urinary tract infections, sepsis), HIV-1 and dengue virus infections, as well as Alzheimer's disease.
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Dolutegravir sodium
0 ImagesSynonyms: S/GSK1349572 sodiumDolutegravir sodium (S/GSK1349572 sodium) 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 sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
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1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide
0 ImagesSynonyms: BMIM-TFSI; BMI-TFSI1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide (BMIM-TFSI; BMI-TFSI) is an HIV-1 integrase inhibitor. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide weakly inhibits recombinant HIV-1 integrase 3'-processing or strand transfer activity. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide can be used for the research of HIV-1.
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Equisetin
0 ImagesEquisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects.
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Cabotegravir sodium
0 ImagesSynonyms: GSK-1265744 sodium; S/GSK1265744 sodiumCabotegravir (GSK-1265744) sodium 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 sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS.
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Pirmitegravir
0 ImagesSynonyms: STP0404Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.
