DENV-IN-4

DENV-IN-4 is a potent DENV inhibitor (DENV EC50=4.79 μM, Vero CC50>100 μM, SI>20.9). DENV-IN-4 can inhibit the expression level of DENV2 with concentration-dependence and reduce RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 has antiviral effect[1].

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

EC50=4.79 μM (DENV)[1]

DENV-IN-4 (compound 15) (0.064-200 μM; 3 days) has antiviral effect and not related to its toxicity (DENV EC50=4.79 μM, Vero CC50>100, SI>20.9)[1]. DENV-IN-4 (3.125-50 μM in Vero, 3.75-30 μM in A549 and Huh-7; 48 hours) inhibits the expression level of DENV2 with concentration-dependence, and inhibition curves were smoother in Vero[1]. DENV-IN-4 (7.5 and 15 μM; 48 hours) can effectively inhibit DENV infection in Vero cells, and completely inhibited at 15 μM[1]. DENV-IN-4 (0-15 μM; 48 hours) inhibits DENV2 E protein production with good concentration-dependent relationship in Vero cells[1]. Cell Cytotoxicity Assay Cell Line: Vero[1] Concentration: 0.064-200 μM Incubation Time: 3 days Result: Showed antiviral effect of DENV-IN-4 was not related to its toxicity (Vero EC50=4.79 μM, CC50>100, SI>20.9). RT-PCR Cell Line: Vero, A549 and Huh-7 cells[1] Concentration: 3.125-50 μM in Vero, 3.75-30 μM in A549 and Huh-7 Incubation Time: 48 hours Result: Inhibited the expression level of DENV2 with concentration-dependence, and inhibition curves were smoother in Vero. Western Blot Analysis Cell Line: Vero[1] Concentration: 7.5 and 15 μM Incubation Time: 48 hours Result: Effectively inhibited DENV infection and completely inhibited at 15 μM. Immunofluorescence Cell Line: Vero[1] Concentration: 0-15 μM Incubation Time: 48 hours Result: Inhibited DENV2 E protein production with good concentration-dependent relationship.

[1]. Qian W, et al. Design, synthesis, discovery and SAR of the fused tricyclic derivatives of indoline and imidazolidinone against DENV replication and infection [published online ahead of print, 2022 Jan 24]. Bioorg Chem. 2022;120:105639.