GS-9160
GS-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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- CAS No.: 915407-80-6
- Formule: C20H18FN3O4S
- Masse moléculaire:415.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
GS-9160 (range; 30 min) potently inhibits purified HIV-1 integrase strand transfer activity with an IC50 of 28 nM[1].
GS-9160 (5 days) potently inhibits HIV-1 IIIb replication in MT-2 cells with an EC50 of 2.1 nM and a selectivity index of 1,905[1].
GS-9160 (5 days) potently inhibits HIV-1 IIIb replication in MT-4 cells with an EC50 of 0.7 nM and a selectivity index of 457[1].
GS-9160 (5 days) potently inhibits HIV-1 BaL replication in primary human CD4-positive T lymphocytes with an EC50 of 1.5 nM and a selectivity index of 2,667[1].
GS-9160 (tested doses; period sufficient for viral replication and circle formation) blocks HIV-1 integration in SupT1 cells, as evidenced by a 1.9-fold increase in 2-LTR circle levels, with a cytotoxicity CC50 of 600 nM[1].
GS-9160 (48 h) specifically inhibits HIV-1 integration in SupT1 cells, reducing integration junctions with an EC50 of 0.9 nM without affecting late reverse transcription product accumulation[1].
GS-9160 potently inhibits HIV replication in vitro, though its activity is reduced in human serum, and it selects for HIV-1 integrase mutations integraseE92V and integraseL74M that are shared with other integrase strand transfer inhibitors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MT-2 T-lymphoblastoid cells
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Concentration:serially diluted (nine concentrations)
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Incubation Time:5 days
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Result:Exhibited potent anti-HIV-1 activity with a mean EC50 of 2.1 nM and a selectivity index (CC50/EC50) of 1,905, with a mean CC50 of 4,000 nM.
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Cell Line:MT-4 T-lymphoblastoid cells
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Concentration:serially diluted (nine concentrations)
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Incubation Time:5 days
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Result:Potently inhibited HIV-1 IIIb replication with a mean EC50 of 0.7 nM and a selectivity index of 457, with a mean CC50 of 320 nM.
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Cell Line:MT-2 cells, primary human CD4-positive T lymphocytes
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Concentration:serially diluted; serum conditions included 10%, 20%, 35%, 50% human serum, or HSA + α1-AGP
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Incubation Time:5 days
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Result:Increased the EC50 7.1-fold to 15 nM in MT-2 cells treated with HSA and α1-AGP, while 100% extrapolated human serum increased the EC50 6-fold to 12 nM.
Increased the EC50 10-fold to 15 nM in primary human T cells treated with HSA + α1-AGP.
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Cell Line:SupT1 cells
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Concentration:tested doses
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Incubation Time:period sufficient for viral replication and circle formation
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Result:Resulted in an approximate 1.9-fold increase in 2-LTR circle levels, indicating blocked HIV-1 integration, with a mean CC50 of 600 nM.
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Cell Line:MT-2 cells
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Concentration:serially diluted combination concentrations
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Incubation Time:5 days
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Result:Showed highly synergistic activity with all tested antiretrovirals, with MacSynergy II volumes ranging from 153.7 to 410.5 nM2·% and CI values ranging from 0.373 to 0.751, consistent with synergism or moderate synergism.
Chemical Information
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CAS No. 915407-80-6
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Masse moléculaire 415.44
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Formule C20H18FN3O4S
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SMILES
O=C1C=2C(O)=C3N=CC=CC3=C(C2CN1CC4=CC=C(F)C=C4)N(C)S(=O)(=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Jones GS, et al. Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. Antimicrobial agents and chemotherapy. 2009 Mar;53(3):1194-203. [Content Brief]
[2]. Choi E, et al. Recent advances in the discovery of small-molecule inhibitors of HIV-1 integrase. Future Sci OA. 2018 Sep 6;4(9):FSO338. [Content Brief]
[3]. Alian A, et al. Catalytically-active complex of HIV-1 integrase with a viral DNA substrate binds anti-integrase drugs. Proceedings of the National Academy of Sciences of the United States of America. 2009 May 19;106(20):8192-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GS-9160 Related Classifications
HY-184318 Related Classifications
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- GS-9160
- 915407-80-6
- GS9160
- GS 9160
- HIV Integrase
- HIV
- primary human CD4-positive T lymphocytes
- HIV-1 integrase mutations
- MT-2 cells
- nonnucleoside reverse transcriptase inhibitors
- MT-4 cells
- primary human T lymphocytes
- HIV-1 protease inhibitors
- SupT1 cells
- HIV-1 integrase
- nucleoside/nucleotide reverse transcriptase inhibitors
- Inhibitor
- inhibitor
- inhibit