JTK-853

JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.

Signaling Pathways >> Anti-infection >> HCV

Research Areas >> Infection

HCV polymerase[1] EC50: 0.38 μM (1a H77 HCV), 0.035 μM (1b Con1 HCV)[1]

JTK-853 is a novel, non-nucleoside Hepatitis C Virus Polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively. When JTK-853 is incubated with the replicon cells for 48 h, it shows antiviral activity against genotype 1a H77 and 1b Con1 replicon cells with EC90 values of 6.5±0.5 and 0.34±0.05 µM, respectively. At 10 µM, JTK-853 induces apparent Huh-7.5 cell death in 2-week culture. JTK-853 suppresses the drug-resistant colony formation in the genotype 1a replicon cells, and the numbers of JTK-853-resistant colonies are much lower than those of GS-9190-resistant colonies for both genotypes[1].

For the determination of cytotoxicity of JTK-853, the Huh-7.5 cells are treated with JTK-853 for 2 weeks. The thumb pocket NNI-B and NS5Ai are added at 100 µM and 100 nM, respectively. JTK-853 is added at 10 µM. JTK-853-containing medium is changed twice a week. Two weeks after the culture, the cells are stained with crystal violet [1% (v/v) in methanol], and then lysed by the lysis buffer. The cytotoxicity is determined as a measurement of OD 595 nm of the cell lysates[1].

[1]. Ando I, et al. JTK-853, a novel non-nucleoside hepatitis C virus polymerase inhibitor, demonstrates a high genetic barrier to resistance in vitro. Intervirology. 2013;56(5):302-9.

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