Dolutegravir (GSK1349572)

For research use only.

Catalog No.S2667 Synonyms: S/GSK1349572

16 publications

Dolutegravir (GSK1349572) Chemical Structure

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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10mM (1mL in DMSO) USD 450 In stock
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Selleck's Dolutegravir (GSK1349572) has been cited by 16 publications

3 Customer Reviews

  • 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.

  • qPCR kinetics of 2-LTRc and integrated DNA forms during a single round of HIV replication in the presence of inhibitors. MT4cells were infected with HIV-1 in the absence (DMSO) or in the presence of 100 nM EFV, 500 nM RAL, 500 nM DTG, 10 μM RDS1611, 10 μM RDS1644, 10 μM RDS1823 added at the time of infection (black bar) or 16 h p.i. (grey bar). Samples were analyzed for (A) total viral DNA at 24 h and (B) 2-LTRc and (C) integrated viral DNA at 48 h. The graph represents the average and standard deviation of three independent experiments. Significant at: p value < 0.05 (*); p value < 0.01 (**); p value < 0.001 (***); p value < 0.0001 (****).

    Antiviral Res, 2016, 134:236-243. 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.

Purity & Quality Control

Choose Selective Integrase Inhibitors

Biological Activity

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.
HIV integrase [2]
(Cell-free assay)
2.7 nM
In vitro

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. [1] 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. [2] 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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDCK2 cells NU\zfXZuTnWwY4Tpc44h[XO|YYm= M1zxWmlvcGmkaYTpc44hd2ZiaIXtZY4hV0OWMjDlfJBz\XO|ZXSgbY4hVUSFS{KgZ4VtdHNidYPpcochYzF2Q23t[ZRnd3KvaX6gZZMhe3Wkc4TyZZRmKGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nz NI[1WWwzOzF|MkOzOC=>

... Click to View More Cell Line Experimental Data


Kinase Assay:


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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.
Cell Research:


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  • Cell lines: MT-4
  • Concentrations: 0 to 10 μM
  • Incubation Time: 4 days or 5 days
  • Method:

    MT-4 cells growing exponentially at a density of 500000 or 600000 /mL are infected with HIV-1 strain IIIB at a viral multiplicity of infection of 0.001 or a 50% tissue culture infective dose of 4 to 10. The cells are then aliquoted to 96-well plates in the presence of varying concentrations of S/GSK1349572. After incubation for 4 or 5 days, antiviral activity is determined by a cell viability assay that either measured bioluminescence with a CellTiter-Glo luminescent reagent or measured absorbance at 560 and 690 nm using the yellow tetrazolium MTT reagent [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide].

    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL warmed (197.91 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 419.38


CAS No. 1051375-16-6
Storage powder
in solvent
Synonyms S/GSK1349572
Smiles CC1CCOC2CN3C=C(C(=O)NCC4=C(F)C=C(F)C=C4)C(=O)C(=C3C(=O)N12)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04166474 Not yet recruiting Drug: Dolutegravir Hiv|Tuberculosis Helen Reynolds|Infectious Disease Institute Kampala Uganda|Desmond Tutu HIV Centre|University of Liverpool April 2020 Phase 4
NCT03851588 Recruiting Other: Placebo|Drug: Dolutegravir 50 mg HIV Infections|Tuberculosis University of Cape Town|Wellcome Trust|Medecins Sans Frontieres Netherlands December 19 2019 Phase 2
NCT04133012 Not yet recruiting Other: Samplings HIV-1 Infection French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|ViiV Healthcare November 1 2019 Not Applicable
NCT04034862 Not yet recruiting Drug: Treatment simplification (dolutegravir lamivudine) HIV Infections University of Liege October 1 2019 Phase 3

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Integrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID