MK-2048 

MK-2048 is a HIV-1 and HIV-1 integrase inhibitor. MK-2048 shows selective activity against HTLV-1-infected cells and retained potency against HIV-1 variants. MK-2048 induces apoptosis, inhibits cell growth, reduces proviral loads, and blocks HTLV-1 transmission and immortalization. MK-2048 can be used for the research of HIV-1 infection^[1][2][3][4].

MK-2048 potently inhibits the growth of HTLV-1-infected cell lines and ATL-derived cell lines^[1].
MK-2048 induces apoptosis in HTLV-1-infected cell lines through activation of the PERK-eIF2a-ATF4 UPR pathway and upregulation of pro-apoptotic markers CHOP and cleaved PARP^[1].
MK-2048 upregulates the PERK-mediated UPR pathway in HTLV-1-infected cell lines and ATL-derived cell lines, leading to activation of pro-apoptotic signaling^[1].
MK-2048 (4 h pre-incubation) potently inhibits cell-free HTLV-1 infection of 293T cells with an EC₅₀ of 1 nM, with no associated cell toxicity^[2].
MK-2048 (0.25-1 nM; 6 days) significantly inhibits cell-to-cell HTLV-1 infection of B5Luc cells at concentrations similar to those active in cell-free infection assays^[2].
MK-2048 (1-10 nM; 10 days) dose-dependently reduces HTLV-1 integration and total viral DNA levels in Jurkat cells, with complete inhibition of integration at concentrations ≥2 nM^[2].
MK-2048 (4 h) inhibits HTLV-1 infection of 293T cells at the stage of viral integration, without affecting reverse transcription^[2].
MK-2048 (0.0256 nM-2 μM; 72 h) inhibits wild-type NL4-3 HIV-1 replication in PM1 cells with an EC₅₀ of 0.0019 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

461.87

C₂₁H₂₁ClFN₅O₄

869901-69-9

Solid

Light yellow to yellow

FC1=C(Cl)C=C(CN2C(C(C(O)=C3N4[C@@H](C)CN(CC)C3=O)=C4C(C(NC)=O)=N2)=O)C=C1

Room temperature in continental US; may vary elsewhere.

• [1]. Ikebe E, et al. PS932 HIV INTEGRASE INHIBITOR MK-2048 INDUCES APOPTOSIS IN HTLV-1 INFECTED CELLS THROUGH THE UPR ACTIVATION[J]. HemaSphere, 2019, 3(S1): 420.

  [2]. Seegulam ME, et al. Integrase inhibitors effective against human T-cell leukemia virus type 1. Antimicrob Agents Chemother. 2011;55(5):2011-2017.

  [3]. Bar-Magen T, et al. Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor. J Virol. 2010;84(18):9210-9216.

  [4]. Tong X, et al. Development and Evaluation of Nanoparticles-in-Film Technology to Achieve Extended In Vivo Exposure of MK-2048 for HIV Prevention. Polymers (Basel). 2022;14(6):1196. Published 2022 Mar 16.