2. Metabolic Enzyme/Protease Anti-infection
  3. HIV Integrase HIV
  4. 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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GS-9160

GS-9160 Chemical Structure

CAS No. : 915407-80-6

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GS-9160 Related Antibodies

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Description

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[1][2][3].

In Vitro

GS-9160 (range; 30 min) potently inhibits purified HIV-1 integrase strand transfer activity with an IC50 of 28 nM[1].
GS-9160 (serially diluted; 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 (serially diluted; 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 (serially diluted; 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 (tested doses; 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 (nanomolar range) 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.

GS-9160 Related Antibodies

Cell Viability Assay[1]

Cell Line: MT-2 T-lymphoblastoid cells
Concentration: serially diluted (nine concentrations)
Incubation Time: 5 days
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.

Cell Viability Assay[1]

Cell Line: MT-4 T-lymphoblastoid cells
Concentration: serially diluted (nine concentrations)
Incubation Time: 5 days
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.

ELISA Assay[1]

Cell Line: MT-2 cells, primary human CD4-positive T lymphocytes
Concentration: serially diluted; serum conditions included 10%, 20%, 35%, 50% human serum, or HSA + α1-AGP
Incubation Time: 5 days
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.

Real Time qPCR[1]

Cell Line: SupT1 cells
Concentration: tested doses
Incubation Time: period sufficient for viral replication and circle formation
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.

Cell Viability Assay[1]

Cell Line: MT-2 cells
Concentration: serially diluted combination concentrations
Incubation Time: 5 days
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.
Molecular Weight

415.44

Formula

C20H18FN3O4S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GS-9160 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GS-9160915407-80-6GS9160GS 9160HIV IntegraseHIVHuman immunodeficiency virusprimary human CD4-positive T lymphocytesHIV-1 integrase mutationsMT-2 cellsnonnucleoside reverse transcriptase inhibitorsMT-4 cellsprimary human T lymphocytesHIV-1 protease inhibitorsSupT1 cellsHIV-1 integrasenucleoside/nucleotide reverse transcriptase inhibitorsInhibitorinhibitorinhibit

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