MK-0536
MK-0536 is a highly potent HIV-1 integrase inhibitor that effectively suppresses the replication of wild-type viruses. MK-0536 retains significant antiviral activity against multiple key drug-resistant mutants such as Y143R and N155H, and shows no toxicity to uninfected cells. MK-0536 selectively blocks the strand transfer reaction of integrase by chelating magnesium ions at the active site and interacting with viral DNA and enzyme residues. MK-0536 is applicable to the study of HIV infection mechanisms.
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- CAS No.: 865298-81-3
- Formule: C19H19ClFN3O4
- Masse moléculaire:407.83
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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HIV-1 |
In Vitro
MK-0536 (0.6 nM-37 μM; 2 h) potently inhibits both strand transfer and 3'-processing activities of wild-type HIV-1 integrase in vitro, with an IC50 of 33 nM for strand transfer and 5.8 μM for 3'-processing[1].
MK-0536 (0.6 nM-37 μM; 2 h) is hypersensitive against HIV-1 integraseY143R, inhibiting strand transfer with an IC50 of 9.5 nM and 3'-processing with an IC50 of 1.4 μM[1].
MK-0536 (0.6 nM-37 μM; 2 h) retains potent activity against HIV-1 integrase, inhibiting strand transfer with an IC50 of 40 nM and 3'-processing with an IC50 of 3.9 μM[1].
MK-0536 (0.6 nM-37 μM; 2 h) exhibits reduced but still significant activity against HIV-1 integrase, inhibiting strand transfer with an IC50 of 237 nM and 3'-processing with an IC50 of 8.3 μM[1].
MK-0536 inhibits wild-type HIV-1 replication in HOS cells with an EC50 of 17 nM and is non-cytotoxic to HeLa cells at concentrations up to 333 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HeLa cell
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Concentration:333 μM
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Incubation Time:24 h
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Result:Showed non-cytotoxic to HeLa cells at 333 μM.
Chemical Information
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CAS No. 865298-81-3
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Masse moléculaire 407.83
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Formule C19H19ClFN3O4
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SMILES
O=C1C(O)=C2C(=O)N(CC3=CC=C(F)C(Cl)=C3)CCC2=C(C(=O)N(C)C)N1C
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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.
Protocole
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-0536 Related Classifications
HY-123883 Related Classifications
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