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^[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 integrase^Y143R, 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.

407.83

C₁₉H₁₉ClFN₃O₄

865298-81-3

O=C1C(O)=C2C(=O)N(CC3=CC=C(F)C(Cl)=C3)CCC2=C(C(=O)N(C)C)N1C

Room temperature in continental US; may vary elsewhere.

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

• [1]. Métifiot M, et al. MK-0536 inhibits HIV-1 integrases resistant to raltegravir. Antimicrob Agents Chemother. 2011;55(11):5127-5133.  [Content Brief]