G243-1720 is a potent, specific anti-poxvirus inhibitor with broad activity in vitro and in vivo, blocks the formation of extracellular enveloped virions and cell-cell spread, affecting dimerization of protein OPG57 (F13).
G243-1720 significantly inhibits the rdMPXVΔ96,158 infection in both HaCaT-96,158 and CV-1-96,158 cells with IC50 of 142 nM.
G243-1720 has an EC50 of 0.194 μM in Vero E6 cells infected with wild-type MPXV in plaque assays.
G243-1720 effectively inhibits VACV replication in these cell lines, with EC50 values ranging from 0.15 to 1.5 μM.
G243-1720 exhibits inhibitory effect on the replication of other orthopoxviruses like CPXV-BR, CPXV-E, CMLV, and RPXV, but not FPV (a member of the distantly related Avipoxvirus genus), HSV-1 (herpes simplex virus type 1), and the RNA viruses VSV (vesicular stomatitis virus) and SINV (Sindbis virus).
G243-1720 specifically inhibits the replication of orthopoxviruses.
G243-1720 via the intraperitoneal (i.p., 22.5 mg/kg) or intragastric (i.g., 45 mg/kg) route reduced the median viral titers from 5.48 logs in SCID mice infected with MPXV.
G243-1720 significantly inhibited infection at the post-entry or entire infection period but not during entry, impacts IEV formation and EEV release, which are critical for the long range spread of the orthopoxviruses.