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Integrase Inhibitors (6)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2005 Raltegravir (MK-0518) Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively.
  • Nature, 2016, 530(7590):358-61
  • Nucleic Acids Res, 2016, 44(14):6896-906
  • Sci Signal, 2015, 8(399):ra104
S2001 Elvitegravir (GS-9137, JTK-303) Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
  • Sci Transl Med, 2014, 6(262):262ra157
  • Cancer Res, 2012, 72(23):6200-8
  • Nucleic Acids Res, 2016, 44(14):6896-906
S2667 Dolutegravir (GSK1349572) 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.
  • Nucleic Acids Res, 2016, 44(14):6896-906
  • J Biol Chem, 2014, 289(28):19648-58
  • Retrovirology, 2015, 10.1186/s12977-015-0146-8
S1366 BMS-707035 BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
S2765 MK-2048 MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
S7766 Cabotegravir (GSK744, GSK1265744) Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S2005 Raltegravir (MK-0518) <1 mg/mL 88 mg/mL <1 mg/mL
S2001 Elvitegravir (GS-9137, JTK-303) <1 mg/mL 90 mg/mL 35 mg/mL
S2667 Dolutegravir (GSK1349572) <1 mg/mL 83 mg/mL <1 mg/mL
S1366 BMS-707035 <1 mg/mL 38 mg/mL <1 mg/mL
S2765 MK-2048 <1 mg/mL 9 mg/mL <1 mg/mL
S7766 Cabotegravir (GSK744, GSK1265744) <1 mg/mL 38 mg/mL <1 mg/mL
Tags: Integrase activity | Integrase inhibitors mechanism | HIV Integrase inhibitor mechanism | Integrase assay | HIV Integrase assay | Integrase inhibitor drugs | HIV Integrase inhibitor drugs | Integrase inhibitor resistance testing | Integrase inhibitor review
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