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MK-2048

CAS No. : 869901-69-9

Biological Activity：MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
IC50 Value: 2.6 nM for HIV Integrase
Target: HIV Integrase
MK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection. MK-2048 inhibits subtype B and subtype C integrase activities. MK-2048 inhibits R263K mutants slightly more effectively than G118R mutants. MK-2048 inhibits S217H intasome and, by contrast, MK-2048 remains fully active against the N224H intasome. MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. MK-2048 is active against viruses resistant to RAL and EVG. MK-2048 exposure leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. MK-2048, with continued pressure, subsequently leads to an additional substitution, at position E138K, after 29 weeks, within the IN gene. Although the G118R mutation alone confers only slight resistance to MK-2048 but not to RAL or EVG, its presence arouses a dramatic reduction in viral replication capacity compared to wild-type NL4-3. E138K both partially restores viral replication capacity and also contributes to increased levels of resistance against MK-2048.

Research Area：Infection

Targets：HIV Integrase|HIV

Related Small Molecules:HIV-1 TAT (48-60);Seletracetam lithium;HIV-IN-2;Triptonine B;FC131;Peritassine A;Flavopiridol;TAT (48-57);FGI-106 tetrahydrochloride;(Z)-9-Propenyladenine;Apabetalone;Decanoyl-RVKR-CMK TFA;ONX-0914 TFA;Apelin-36(rat, mouse);Ulonivirine;Islatravir;HIV-1 inhibitor-19

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