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Cat. No.: HY-182277

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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.

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CAS No.: 1392118-63-6
화학식: C₂₆H₂₈FNO₅
분자량:453.50

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

GSK-1264 Chemical Structure

CAS No.: 1392118-63-6

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

Biological Activity
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- In Vitro
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Bioz

Biological Activity

제품 설명

All HIV Isoforms :

In Vitro

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 IN^Y15A,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

CAS No. 1392118-63-6
분자량 453.50
화학식 C₂₆H₂₈FNO₅
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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Gupta K, et al. Structural Basis for Inhibitor-Induced Aggregation of HIV Integrase. PLoS Biol. 2016;14(12):e1002584. Published 2016 Dec 9. [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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100 mg

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Biological Activity
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GSK-1264

All HIV Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

GSK-1264 Related Classifications

HY-182277 Related Classifications