Cat. No.: HY-184318

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.

For research use only. We do not sell to patients.

CAS No.: 915407-80-6
Formula: C₂₀H₁₈FN₃O₄S
Molecular Weight:415.44

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

GS-9160 Chemical Structure

CAS No.: 915407-80-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
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Classifications
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Biological Activity

Description

All HIV Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Lymphocyte	EC₅₀	1.5 nM Compound: GS-9160	Antiviral activity against 0.001 MOI HIV1 BAL infected in human T lymphocyte cells by p24 antigen ELISA in presence of 10% FBS Antiviral activity against 0.001 MOI HIV1 BAL infected in human T lymphocyte cells by p24 antigen ELISA in presence of 10% FBS	[PMID: 19104010]
Lymphocyte	EC₅₀	15 nM Compound: GS-9160	Antiviral activity against 0.001 MOI HIV1 BAL infected in human T lymphocyte cells by p24 antigen ELISA in presence of 10% FBS, HSA and alpha1-AGP Antiviral activity against 0.001 MOI HIV1 BAL infected in human T lymphocyte cells by p24 antigen ELISA in presence of 10% FBS, HSA and alpha1-AGP	[PMID: 19104010]
Lymphocyte	CC₅₀	4000 nM Compound: GS-9160	Cytotoxicity against human T lymphocyte cells infected with HIV1 BAL by XTT method in presence of 10% FBS Cytotoxicity against human T lymphocyte cells infected with HIV1 BAL by XTT method in presence of 10% FBS	[PMID: 19104010]
MT2	EC₅₀	1.7 nM Compound: 2	Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of fetal bovine serum Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of fetal bovine serum	[PMID: 19285389]
MT2	EC₅₀	11.4 nM Compound: 2	Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of human serum albumin Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of human serum albumin	[PMID: 19285389]
MT2	EC₅₀	2.1 nM Compound: GS-9160	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT2	EC₅₀	15 nM Compound: GS-9160	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, HSA and alpha1-AGP Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, HSA and alpha1-AGP	[PMID: 19104010]
MT2	EC₅₀	12 nM Compound: GS-9160	Antiviral activity against 0.01 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum Antiviral activity against 0.01 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum	[PMID: 19104010]
MT2	CC₅₀	4000 nM Compound: GS-9160	Cytotoxicity against human MT2 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS Cytotoxicity against human MT2 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT2	EC₅₀	19 nM Compound: GS-9160	Antiviral activity against 0.02 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum Antiviral activity against 0.02 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum	[PMID: 19104010]
MT2	EC₅₀	30 nM Compound: GS-9160	Antiviral activity against 0.04 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum Antiviral activity against 0.04 MOI HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 100% human serum	[PMID: 19104010]
MT4	EC₅₀	0.7 nM Compound: GS-9160	Antiviral activity against HIV1 3B infected in human MT-4 cells by two fold dilution method in presence of 10% FBS Antiviral activity against HIV1 3B infected in human MT-4 cells by two fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT4	CC₅₀	320 nM Compound: GS-9160	Cytotoxicity against human MT4 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS Cytotoxicity against human MT4 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS	[PMID: 19104010]
SUP-T1	CC₅₀	600 nM Compound: GS-9160	Cytotoxicity against human SupT1 cells infected with HIV1 3B Cytotoxicity against human SupT1 cells infected with HIV1 3B	[PMID: 19104010]
SUP-T1	EC₅₀	1000 nM Compound: GS-9160	Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs	[PMID: 19104010]
SUP-T1	EC₅₀	0.9 nM Compound: GS-9160	Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay	[PMID: 19104010]

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 (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 integrase^E92V and integrase^L74M 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.

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.

Chemical Information

CAS No. 915407-80-6
Molecular Weight 415.44
Formula C₂₀H₁₈FN₃O₄S
SMILES

O=C1C=2C(O)=C3N=CC=CC3=C(C2CN1CC4=CC=C(F)C=C4)N(C)S(=O)(=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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GS-9160

All HIV Isoforms