Urea, N-[4-(4-butyl-1H-1,2,3-triazol-1-yl)phenyl]-N'-(2-methylphenyl)-

Biological Activity

DDX3-IN-2 is an active DEADbox polypeptide 3 (DDX3) inhibitor with an IC50 value of 0.3 μM. DDX3-IN-2 shows a broad spectrum of antiviral activity. DDX3-IN-2 has the potential to overcome HIV resistance[1]. DDX3-IN-2 behaves as a competitive inhibitor with respect to the RNA substrate, which can be seen by the decrease in its inhibition potency as a function of increasing RNA substrate concentrations. DDX3-IN-2 is found to be completely inactive against the ATPase of DDX3, DDX1 helicase, and DENV NS3 helicase[1]. DDX3-IN-2 (20 mg/kg; tail vein injection) possesses excellent biocompatibility, and Wistar rats shows a good tolerance to the dose of 20 mg/kg[1].DDX3-IN-2 (10 mg/kg; i.v. bolus injection; 0~25 hours) rapidly eliminates the half-life elimination and the plasmatic clearance values[1].

References

[1]. Brai A, et al. Human DDX3 protein is a valuable target to develop broad spectrum antiviral agents. Proc Natl Acad Sci U S A. 2016;113(19):5388-5393.