Treatment with the FIT-039 ointment twice a day suppresses skin lesions and rescues mice (male BALB/c mice injected with HSV-1) from lethality in a dose-dependent manner. The healing of lesions is observed with 5% to 10% FIT-039 ointment, leading to the complete regression of zosteriform spread on day 10, which is also observed with the 5% ACV ointment[1]. FIT-039 does not affect body weight gain in mice administrated with an overdose of this compound (1000 mg/kg/d) for 14 days, and no changes are observed in biological markers in their blood[1].
In Vitro
FIT-039 (30 μM; 3 hours; HEK293 cells) treatment decreases phosphorylated CTD in the infected or noninfected cells to a level lower than that shown by Flavopiridol. FIT-039 reduces the expression levels of HSV-1 immediate-early genes (IEGs) and early and late genes[1]. FIT-039 inhibits replication of the HSV-1 genome in a dose-dependent manner (EC50 and EC80 are 0.69 μM and 4.0 μM, respectively)[1]. FIT-039 potently suppresses 8 kinases (GSK3β, PKN1, haspin, p70s6K, DYRK1B, GSK3α, IRR, and DYRK3) other than CDK9 on the 332-kinase panel. These kinases are involved in the replication of various viruses[1]. Western Blot Analysis[1] Cell Line: HEK293 cells Concentration: 30 μM Incubation Time: 3 hours Result: Decreased phosphorylated carboxyterminal domain (CTD) in the infected or noninfected cells to a level lower than that shown by Flavopiridol.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Makoto Yamamoto, et al. CDK9 Inhibitor FIT-039 Prevents Replication of Multiple DNA Viruses. J Clin Invest. 2014 Aug;124(8):3479-88.
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