GSK-1264
GSK-1264 is an HIV-1 integrase inhibitor. GSK-1264 binds to a site spanning the HIV-1 integrase catalytic core domain and C-terminal domain, mediates formation of an open polymer of HIV-1 integrase dimers via inhibitor-bridged contacts between adjacent dimers. GSK-1264 disrupts late-stage HIV replication by interfering with viral particle assembly. GSK-1264 stimulates inappropriate polymerization of HIV-1 integrase. GSK-1264 can be used for the research of HIV infection.
For research use only. We do not sell to patients.
- CAS No.: 1392118-63-6
- Formula: C26H28FNO5
- Molecular Weight:453.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
GSK1264 (100-1000 nM; 96 h) potently disrupts formation of mature HIV-1 particles in chronically infected A1953 cells, significantly reducing the percentage of mature virions and increasing deformed particles[1].
GSK1264 (0.5-1.0 mM) binds to a bipartite interface formed by the CTD and CCD of adjacent HIV-1 INY15A,D185A dimers, inducing formation of an open polymer structure at 4.4 Å resolution[1].
GSK1264 (8-10 μM) induces concentration-dependent aggregation of HIV-1 IN fragments containing both CCD and CTD domains in vitro, and this activity requires specific CTD residues at the GSK1264 binding interface[1].
GSK1264 (7 days) inhibits replication of diverse primary HIV-1 isolates in PBMCs with IC50 values of 2-100 μM, and naturally occurring IN polymorphisms can modulate its potency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1392118-63-6
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Molecular Weight 453.50
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Formula C26H28FNO5
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SMILES
CC(C)(C)O[C@@H](C1=C(C2=CC(F)=C(OCCC3)C3=C2C)C4=CC=CC=C4C(N1C)=O)C(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-1264 Related Classifications
HY-182277 Related Classifications
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