Catalog No.S2667 Synonyms: S/GSK1349572
Molecular Weight(MW): 419.38
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
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Strand transfer was carried out with RSV IN(1-269) (4 uM) and GU320R(2 uM)in the presence of 50mM NDSB201. Increasing concentrations of STIs were added as indicated at the top; DTG(Dolutegravir) in lanes 3-5, MK-2048 in lanes 6-8, and RAL in lanes 9-11. No STI was present in lane 2, and lane 1 contains the molecular weight markers. Strand transfer products and ODN substrate are identified on the right. CHS, circular half-site; OC target and SC target, open circular and supercoiled target DNA, respectively.
J Biol Chem 2014 289(28), 19648-58. Dolutegravir (GSK1349572) purchased from Selleck.
Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. The number of independent determinations (n) for each strain is shown below the x-axis. No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.
Retrovirology, 2015, 10.1186/s12977-015-0146-8. Dolutegravir (GSK1349572) purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
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|Description||Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.|
|Features||A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.|
S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-naive HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM.  In vitro, S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM. Furthermore, S/GSK1349572 potently inhibits HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector with EC50 of 0,51 nM, 0.71 nM and 2.2 nM, respectively.  In vitro, S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses with EC50 ranging from 1.3 nM -2.1 nM. Similarly to that against wild-type virus, S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses with EC50 of 0.36 nM and 0.37 nM, respectively. 
In vitro strand transfer assay:The inhibitory potencies of S/GSK1349572 and other INIs are measured in a strand transfer assay using recombinant HIV integrase. A complex of integrase and biotinylated preprocessed donor DNA-streptavidin-coated Acintillation proximity assay (SPA) beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA-4 mg/mL streptavidin-coated SPA beads in 25 mM sodium morpholinepropanesulfonic acid (MOPS) (pH 7.2), 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37 °C. These beads are spun down and preincubated with diluted INIs for 60 minutes at 37 °C. Then a 3H-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction mixture is incubated at 37 °C for 25 to 45 minutes, which allows for a linear increase in the strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
|In vitro||DMSO||83 mg/mL (197.91 mM) warming|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02777229||Recruiting||HIV-1 Infection||French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut de Recherche pour le Developpement||July 2016||Phase 3|
|NCT02831673||Not yet recruiting||Infection, Human Immunodeficiency Virus||ViiV Healthcare|PPD|GlaxoSmithKline||July 2016||Phase 3|
|NCT02831764||Not yet recruiting||Infection, Human Immunodeficiency Virus||ViiV Healthcare|PPD|GlaxoSmithKline||July 2016||Phase 3|
|NCT02738931||Completed||Infection, Human Immunodeficiency Virus||ViiV Healthcare|GlaxoSmithKline||May 2016||Phase 1|
|NCT02771249||Recruiting||Healthy Volunteers||National Institutes of Health Clinical Center (CC)||May 2016||Phase 1|
|NCT02715479||Completed||HIV||Bristol-Myers Squibb||April 2016||Phase 1|
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