MBX2546 is a small molecule inhibitor of influenza virus via targeting influenza hemagglutinin (HA), specifically inhibits HA-mediated viral entry with potent antiviral activity against different influenza virus strains (IC50=0.3-5.9 uM).
MBX2546 binds to HA in a nonoverlapping manner, binds to the group 1 HA-specific conformational epitope in the HA stem region.
MBX2546 displays little inhibitory activity against HIV/LASV-GP, HIV/EBOV-GP, or HIV/VSV-G with IC50 values >100 uM.
MBX2546 inhibitsinfluenza A H1N1 virus strains A/PR/8/34 (H1N1) and A/Florida/21/2008 (H1N1-H275Y) (oseltamivir-resistant strain) with IC50s of 0.3 μM and 5.8 μM, respectively.
MBX2546 also inhibits other H1N1 strains, including A/California/10/2009/H1N1 (2009 pandemic strain), with IC50s of between 0.55 μM and 1.5 μM.
MBX2546 displays significantly less activity against influenza A H3N2 virus strain A/Texas/12/2007 (H3N2) and influenza B virus strain B/Florida/4/2006.
MBX2546 specifically inhibits influenza viruses of group 1 HA (H1 and H5 subtypes), but not group 2 HA (H3 and H7 subtypes).
MBX2546 exhibit strong synergy with oseltamivir.