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.
For research use only. We do not sell to patients.
- CAS No.: 865298-81-3
- Formula: C19H19ClFN3O4
- Molecular Weight:407.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HIV-1 |
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.
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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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Molecular Weight 407.83
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Formula 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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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)